AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: bromocriptine
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.818
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: bromocriptine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.708
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: bromocriptine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.328
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: bromocriptine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.16
Drug: bromocriptine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 8.4
Assay: In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes.
Drug: bromocriptine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.25
Drug: bromocriptine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8
Action type: AGONIST
Drug: bromocriptine
Target: Vesicular glutamate transporter 3 (Transporter)
Gene: Slc17a8
UniProt: Q7TSF2 (VGLU3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.66
Drug: bromocriptine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.5
Action type: AGONIST
Drug: bromocriptine
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.29
Assay: Alpha-2 adrenergic receptor activity assessed in vitro for displacement of [3H]clonidine from specific binding sites on rat striatal membranes
Drug: bromocriptine
Target: Dopamine receptor (GPCR)
Gene: Drd1|Drd3|Drd5|Drd4|Drd2
UniProt: P18901|P19020|P25115|P30729|P61169 (DRD1_RAT|DRD3_RAT|DRD5_RAT|DRD4_RAT|DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.55
Assay: In vitro affinity for dopamine receptor by displacement of [3H]- apomorphine in rat striatal membranes
Drug: bromocriptine
Target: Cerebral cortex alpha adrenergic receptor (GPCR)
Gene: ADRA1A|ADRA2A
UniProt: P18130|Q28838 (ADA1A_BOVIN|ADA2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.29
Assay: In vitro affinity for alpha adrenergic receptor by displacement of 3[H]clonidine in calf cerebral cortex
Drug: bromazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.886
Action type: ANTAGONIST
Drug: bromopride
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Drug: bromopride
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.17
Drug: bromperidol
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: bromperidol
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.43
Action type: ANTAGONIST
Drug: bromperidol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.02
Drug: bromperidol
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Drug: bromperidol
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Drug: bromperidol
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.155
Drug: bromperidol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.119
Drug: bromperidol
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.745
Drug: bromperidol
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.146
Drug: bromperidol
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.77
Drug: bromperidol
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.319
Drug: bromperidol
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Drug: brompheniramine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.05
Assay: Inhibition of human ERG
Drug: brompheniramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.218
Action type: ANTAGONIST
Drug: brompheniramine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.96
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: brotizolam
Target: Platelet-activating factor receptor (GPCR)
Gene: PTAFR
UniProt: P25105 (PTAFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Assay: In vitro for platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets.
Drug: broxyquinoline
Target: Catechol O-methyltransferase (Enzyme)
Gene: Comt
UniProt: P22734 (COMT_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.39
Assay: Inhibition of Sprague-Dawley rat liver COMT after 10 mins using 0.05 uCi [14CH3]-SAM as substrate
Drug: buclizine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL231; SINGLE PROTEIN
Drug: budesonide
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: budesonide
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 10.3
Action type: AGONIST
Drug: budesonide
Target: Interleukin-5 (Cytokine)
Gene: IL5
UniProt: P05113 (IL5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.92
Drug: budesonide
Target: Interferon gamma (Cytokine)
Gene: IFNG
UniProt: P01579 (IFNG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.5
Drug: budesonide
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.85
Action type: AGONIST
Drug: budesonide
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.55
Action type: AGONIST
Drug: budesonide
Target: Matrix metalloproteinase-9 (Enzyme)
Gene: MMP9
UniProt: P14780 (MMP9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.701
Assay: DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2)
Drug: budesonide
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.963
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: budesonide
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.569
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: budesonide
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.54
Assay: Steroid binding against the rat thymus glucocorticoid receptor
Drug: budesonide
Target: Interleukin-5 (Unclassified)
Gene: Il5
UniProt: P04401 (IL5_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.58
Assay: Inhibition of IL5-mediated proliferation of mouse Y16 cells by WST1 assay
Drug: budipine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.07
Assay: Inhibition of human ERG
Drug: budipine
Target: Glutamate [NMDA] receptor (Ion channel)
Gene: GRIN2D|GRIN3B|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN3A
UniProt: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5 (NMDE4_HUMAN|NMD3B_HUMAN|NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMD3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.93
Assay: The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex.
Drug: buflomedil
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Drug: buflomedil
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.89
Assay: Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: buflomedil
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.22
Assay: Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand
Drug: buflomedil
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: buflomedil
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Drug: buflomedil
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Drug: buflomedil
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Drug: buflomedil
Target: Voltage-dependent calcium channel gamma-1 subunit (Ion channel)
Gene: CACNG1
UniProt: Q06432 (CCG1_HUMAN)
Organism: Homo sapiens
Drug: buflomedil
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 5.15
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: bufuralol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Drug: bufuralol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Drug: bufuralol
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: bufuralol
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ks = 4.59
Drug: bumetanide
Target: Solute carrier family 12 member 1 (Transporter)
Gene: SLC12A1
UniProt: Q13621 (S12A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Action type: INHIBITOR
Drug: bumetanide
Target: Sodium/potassium-transporting ATPase subunit alpha-1 (Transporter)
Gene: ATP1A1
UniProt: P05023 (AT1A1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.52
Drug: bumetanide
Target: Solute carrier family 12 member 2 (Transporter)
Gene: SLC12A2
UniProt: P55011 (S12A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.6
Action type: INHIBITOR
Drug: bumetanide
Target: G-protein coupled receptor 35 (GPCR)
Gene: GPR35
UniProt: Q9HC97 (GPR35_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.54
Action type: AGONIST
Drug: bunazosin
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: bunazosin
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Drug: bunazosin
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: bunazosin
Target: Ribosyldihydronicotinamide dehydrogenase [quinone] (Enzyme)
Gene: NQO2
UniProt: P16083 (NQO2_HUMAN)
Organism: Homo sapiens
Drug: levobunolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.399
Action type: ANTAGONIST
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: levobunolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.263
Action type: ANTAGONIST
Assay: DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug: levobunolol
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.488
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: levobunolol
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.585
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: levobunolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.78
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: levobunolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.593
Action type: ANTAGONIST
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: levobunolol
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.54
Drug: levobunolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P25962 (ADRB3_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.3
Action type: ANTAGONIST
Drug: levobunolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P26255 (ADRB3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: bupivacaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.66
Action type: BLOCKER
Drug: bupivacaine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.66
Assay: Inhibition of wild-type human ERG channel expressed in CHO cells by whole-cell patch clamp technique
Drug: bupivacaine
Target: Sodium channel protein type 1 subunit alpha (Ion channel)
Gene: SCN1A
UniProt: P35498 (SCN1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.293
Drug: bupivacaine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: BLOCKER
Drug: bupivacaine
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.514
Drug: bupivacaine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.398
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: bupivacaine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.233
Drug: bupivacaine
Target: Potassium voltage-gated channel subfamily D member 3 (Ion channel)
Gene: KCND3
UniProt: Q9UK17 (KCND3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Drug: bupivacaine
Target: Potassium voltage-gated channel subfamily A member 5 (Ion channel)
Gene: KCNA5
UniProt: P22460 (KCNA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.4
Action type: BLOCKER
Drug: bupivacaine
Target: Potassium channel subfamily K member 3 (Ion channel)
Gene: KCNK3
UniProt: O14649 (KCNK3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.39
Assay: Inhibition of human TASK1 expressed in Xenopus oocytes by whole cell voltage clamp assay
Drug: bupivacaine
Target: Potassium voltage-gated channel subfamily D member 3 (Ion channel)
Gene: Kcnd3
UniProt: Q9Z0V1 (KCND3_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.5
Action type: BLOCKER
Drug: bupranolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: ANTAGONIST
Drug: bupranolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: ANTAGONIST
Drug: bupranolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: buprenorphine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.29
Action type: PARTIAL AGONIST
Drug: buprenorphine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Inhibition of human ERG
Drug: buprenorphine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.01
Action type: ANTAGONIST
Drug: buprenorphine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.07
Action type: ANTAGONIST
Drug: buprenorphine
Target: Nociceptin receptor (GPCR)
Gene: OPRL1
UniProt: P41146 (OPRX_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.11
Assay: Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
Drug: buprenorphine
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.89
Assay: Displacement of [3H]diprenorphine from rat mu opioid receptor expressed in rat C6 cells
Drug: buprenorphine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.4
Assay: Displacement of [3H]DAMGO from MOR in Hartley guinea pig membrane
Drug: buprenorphine
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.32
Assay: Displacement of [3H]diprenorphine from rat delta opioid receptor expressed in rat C6 cells
Drug: buprenorphine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.3
Assay: Displacement of [3H]U69593 from KOR in Hartley guinea pig membrane
Drug: bupropion
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.04
Drug: bupropion
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.16
Action type: INHIBITOR
Assay: Displacement of [125I]RTI55 from cloned human NET expressed in HEK293 cells
Drug: bupropion
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  4.796
Drug: bupropion
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Action type: INHIBITOR
Drug: bupropion
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Drug: bupropion
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Assay: Inhibitory concentration against Nicotinic acetylcholine receptor alpha 7
Drug: bupropion
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: bupropion
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.846
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: bupropion
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.91
Assay: Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand
Drug: bupropion
Target: Neuronal acetylcholine receptor; alpha3/beta4 (Ion channel)
Gene: CHRNB4|CHRNA3
UniProt: P30926|P32297 (ACHB4_HUMAN|ACHA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.74
Assay: Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta4
Drug: bupropion
Target: Neuronal acetylcholine receptor; alpha3/beta2 (Ion channel)
Gene: CHRNB2|CHRNA3
UniProt: P17787|P32297 (ACHB2_HUMAN|ACHA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2
Drug: buserelin
Target: Lutropin-choriogonadotropic hormone receptor (GPCR)
Gene: LHCGR
UniProt: P22888 (LSHR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.569
Drug: buserelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: GNRHR
UniProt: P30968 (GNRHR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 10.52
Action type: AGONIST
Drug: buserelin
Target: Gonadotropin-releasing hormone receptor (GPCR)
Gene: Gnrhr
UniProt: Q01776 (GNRHR_MOUSE)
Organism: Mus musculus
Activity: EC50 = 10.05
Action type: AGONIST
Drug: buspirone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.68
Drug: buspirone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.319
Drug: buspirone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.4
Assay: Inhibition of human ERG
Drug: buspirone
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.13
Drug: buspirone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.25
Action type: PARTIAL AGONIST
Drug: buspirone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.6
Drug: buspirone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.41
Drug: buspirone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.04
Drug: buspirone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.435
Drug: buspirone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.18
Assay: Inhibition of [3H]spiperone binding to Dopamine receptor D3 in bovine cortex
Drug: buspirone
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7