AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: dofetilide
Target: Potassium voltage-gated channel subfamily H member 1 (Ion channel)
Gene: KCNH1
UniProt: O95259 (KCNH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.5
Action type: BLOCKER
Drug: domperidone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.766
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: domperidone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.4
Action type: ANTAGONIST
Drug: domperidone
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.988
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: domperidone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.79
Drug: domperidone
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: domperidone
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.79
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: domperidone
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.586
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: domperidone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.959
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: domperidone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.781
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: domperidone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.156
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: domperidone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.65
Drug: domperidone
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.013
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: domperidone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.46
Assay: Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells
Drug: domperidone
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.807
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: domperidone
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.523
Drug: domperidone
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.833
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: domperidone
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.097
Drug: domperidone
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.936
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: domperidone
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.276
Drug: domperidone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.553
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: domperidone
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Drug: domperidone
Target: Retinoic acid receptor RXR-alpha (Nuclear hormone receptor)
Gene: RXRA
UniProt: P19793 (RXRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.06
Assay: Binding affinity to RXRalpha-LBD (unknown origin) measured up to 120 sec by surface plasma resonance method
Drug: domperidone
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.06
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: domperidone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.55
Drug: domperidone
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.28
Assay: Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Drug: domperidone
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.93
Assay: Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Drug: domperidone
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Drug: domperidone
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: domperidone
Target: Multidrug and toxin extrusion protein 2 (Transporter)
Gene: SLC47A2
UniProt: Q86VL8 (S47A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.83
Assay: Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: donepezil
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.84
Assay: Displacement of [3H]DTG from sigma 1 receptor (unknown origin)
Drug: donepezil
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Assay: Inhibition of human ERG
Drug: donepezil
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.46
Drug: donepezil
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.046
Drug: donepezil
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: INHIBITOR
Drug: donepezil
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.82
Assay: Inhibition of human recombinant MAO-B using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay
Drug: donepezil
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P06276 (CHLE_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.9
Assay: Non competitive inhibition of human serum BChE using butyrylthiocholine iodide as substrate by Lineweaver-Burk plot analysis
Drug: donepezil
Target: Histamine H3 receptor (GPCR)
Gene: HRH3
UniProt: Q9Y5N1 (HRH3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.46
Assay: Inhibition of histamine H3 receptor
Drug: donepezil
Target: Beta-secretase 1 (Enzyme)
Gene: BACE1
UniProt: P56817 (BACE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.49
Assay: Inhibition of BACE1
Drug: donepezil
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: P04058 (ACES_TORCA)
Organism: Torpedo californica
Activity: IC50 = 8.24
Assay: Inhibition of Torpedo californica AChE
Drug: donepezil
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P21836 (ACES_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.24
Assay: Inhibitory activity against acetylcholinesterase
Drug: donepezil
Target: Butyrylcholinesterase; Protein Bche (Enzyme)
Gene: Bche
UniProt: Q9JKC1 (Q9JKC1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.56
Assay: Inhibition of BChE in rat serum after 15 mins by modified Ellman method
Drug: donepezil
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P37136 (ACES_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.77
Assay: In vitro inhibitory effect on rat Acetylcholinesterase
Drug: donepezil
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 7.25
Assay: Non competitive inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Lineweaver-Burk plot analysis
Drug: donepezil
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P23795 (ACES_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.54
Assay: Inhibition of fetal Bovine serum AChE
Drug: donepezil
Target: Choline O-acetyltransferase (Enzyme)
Gene: Chat
UniProt: P32738 (CLAT_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.28
Assay: In vitro inhibitory activity against acetylcholinesterase
Drug: donepezil
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.82
Assay: Inhibition of rat liver mitochondrial MAO-B using [14C]-phenylethylamine after 30 mins by scintillation counting
Drug: donepezil
Target: Cholinesterase (Enzyme)
Gene: Bche
UniProt: Q03311 (CHLE_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.15
Assay: Inhibition of BuChE in mouse brain homogenate using butyrylthiocholine as substrate preincubated for 300 secs followed by substrate addition by Ellman's method
Drug: donepezil
Target: Butyrylcholinesterase (Enzyme)
Gene: BCHE
UniProt: Q9N1N9 (Q9N1N9_HORSE)
Organism: Equus caballus
Activity: Ki = 6.19
Assay: Inhibition of Equine Butyrylcholinesterase
Drug: donepezil
Target: Sigma non-opioid intracellular receptor 1 (Membrane other)
Gene: SIGMAR1
UniProt: Q60492 (SGMR1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.84
Assay: Displacement of [3H]DTG from S1R in P2 fraction of Hartley guinea pig whole brain after 90 mins by liquid scintillation counting method
Drug: donepezil
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: IC50 = 6.08
Assay: Inhibition of equine serum BuChE by Ellman's method
Drug: dopamine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Action type: AGONIST
Drug: dopamine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.19
Assay: Binding affinity to human adrenergic beta2 receptor
Drug: dopamine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: dopamine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: dopamine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.18
Drug: dopamine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.084
Drug: dopamine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: dopamine
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: dopamine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.19
Assay: Displacement of [125I]RT155 binding in HEK cells expressing human DAT
Drug: dopamine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: dopamine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.375
Drug: dopamine
Target: Melatonin receptor type 1A (GPCR)
Gene: MTNR1A
UniProt: P48039 (MTR1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.15
Assay: Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
Drug: dopamine
Target: Melatonin receptor type 1B (GPCR)
Gene: MTNR1B
UniProt: P49286 (MTR1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.04
Assay: Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells
Drug: dopamine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.35
Assay: Displacement of [3H]-spiperone from rat dopamine D2S receptor expressed in rat C6 cells after 45 mins by scintillation counting analysis
Drug: dopamine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.7
Assay: Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry
Drug: dopamine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: Q95136 (DRD1_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.15
Assay: Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug: dopamine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P18090 (ADRB1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5
Assay: Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
Drug: dopamine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.82
Assay: Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug: dopamine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.74
Assay: Binding Affinity on high Affinity Site of Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]pramipexole was tested
Drug: dopamine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P54833 (ADRB2_CANFA)
Organism: Canis familiaris
Activity: Ki = 4.3
Assay: Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug: dopamine
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.96
Assay: Binding affinity which represents concentration giving half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate
Drug: dopamine
Target: D(4) dopamine receptor (GPCR)
Gene: Drd4
UniProt: P30729 (DRD4_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 8.62
Assay: In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug: dopamine
Target: Lysine-specific demethylase 4E (Enzyme)
Gene: KDM4E
UniProt: B2RXH2 (KDM4E_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Drug: dopamine
Target: Dopamine beta-hydroxylase (Enzyme)
Gene: DBH
UniProt: P09172 (DOPO_HUMAN)
Organism: Homo sapiens
Activity: Km = 3
Drug: dopamine
Target: Opioid receptor (GPCR)
Gene: Oprd1|Oprm1|Oprk1|Sigmar1
UniProt: P33533|P33535|P34975|Q9R0C9 (OPRD_RAT|OPRM_RAT|OPRK_RAT|SGMR1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.52
Assay: Ability to inhibit the specific binding of [3H]- dihydromorphine to opiate receptors in rat brain membrane preparation by 50%
Drug: dopamine
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.24
Assay: Binding of [3H]clonidine to alpha-2-adrenergic receptor of rat cerebral cortical membranes
Drug: dopamine
Target: Dopamine receptor (GPCR)
Gene: DRD2|DRD1
UniProt: P20288|Q95136 (DRD2_BOVIN|DRD1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.43
Assay: Tested for binding to dopamine receptor using [3H]- ADTN as radioligand in calf caudate nucleus homogenates.
Drug: dopamine
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 = 5.27
Assay: Tested for Dopamine receptor activity by the inhibition against spiroperidol binding to rat caudate tissue.
Drug: dopamine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.85
Assay: Binding of [3H]prazosin to alpha-1 adrenergic receptor of rat cerebral cortical membranes
Drug: dopamine
Target: Adenylate cyclase (Enzyme)
Gene: Adcy1|Adcy3|Adcy2|Adcy4|Adcy8|Adcy6|Adcy5
UniProt: D4A3N4|P21932|P26769|P26770|P40146|Q03343|Q04400|Q8CFM9 (D4A3N4_RAT|ADCY3_RAT|ADCY2_RAT|ADCY4_RAT|ADCY8_RAT|ADCY6_RAT|ADCY5_RAT|Q8CFM9_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 5.46
Assay: Tested for ability to stimulate dopamine sensitive adenylate cyclase in rat caudate homogenate
Drug: dopamine
Target: Adenosine A2b receptor (GPCR)
Gene: Adora2b
UniProt: P29276 (AA2BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.01
Drug: dopamine
Target: FAD-linked sulfhydryl oxidase ALR (Enzyme)
Gene: GFER
UniProt: P55789 (ALR_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 5.85
Assay: PUBCHEM_BIOASSAY: HTS-Luminescent assay for inhibitors of ALR by detection of hydrogen peroxide production Measured in Biochemical System Using Plate Reader - 2036-02_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488787]
Drug: dopamine
Target: M18 aspartyl aminopeptidase (Enzyme)
UniProt: Q8I2J3 (Q8I2J3_PLAF7)
Organism: Plasmodium falciparum (isolate 3D7)
Activity: IC50 = 5.7
Assay: Active
Drug: dopexamine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Drug: dopexamine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Drug: dorzolamide
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Action type: INHIBITOR
Assay: Inhibition of human recombinant carbonic anhydrase 2 by dansylamide (DNSA) competition assay
Drug: dorzolamide
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: Inhibition of human cloned CA1 by CO2 hydration method
Drug: dorzolamide
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.37
Assay: Inhibition of cloned isozyme, human carbonic anhydrase IV
Drug: dorzolamide
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.28
Assay: Inhibitory activity against human carbonic anhydrase IX (hCA IX) by using CO2 hydrase assay method
Drug: dorzolamide
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.46
Assay: Inhibitory activity against catalytic domain of human carbonic anhydrase XII
Drug: dorzolamide
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.38
Assay: Inhibitory activity against human recombinant mitochondrial isozyme CA VA
Drug: dorzolamide
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.48
Assay: Inhibitory activity against human recombinant mitochondrial isozyme CA VB
Drug: dorzolamide
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.46
Assay: Ki value against human carbonic anhydrase VII
Drug: dorzolamide
Target: Carbonic anhydrase (Enzyme)
Gene: cynT
UniProt: O24855 (CYNT_HELPY)
Organism: Helicobacter pylori (strain ATCC 700392 / 26695)
Activity: Ki = 5.37
Assay: Inhibition of Helicobacter pylori recombinant CA
Drug: dorzolamide
Target: Carbonic anhydrase 3 (Enzyme)
Gene: CA3
UniProt: P07451 (CAH3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Assay: Inhibition of human carbonic anhydrase 3
Drug: dorzolamide
Target: Carbonic anhydrase 6 (Enzyme)
Gene: CA6
UniProt: P23280 (CAH6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Assay: Inhibition of full length human recombinant CA VI
Drug: dorzolamide
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.57
Assay: Inhibitory constant against human carbonic anhydrase XIV in CO2 hydrase assay
Drug: dorzolamide
Target: Carbonic anhydrase 13 (Enzyme)
Gene: Ca13
UniProt: Q9D6N1 (CAH13_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.74
Assay: Inhibitory activity against murine carbonic anhydrase XIII (mCA XIII) by using CO2 hydrase assay method
Drug: dorzolamide
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: Q95323 (CAH4_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.37
Assay: Inhibitory activity against bovine carbonic anhydrase IV from lung microsomes
Drug: dorzolamide
Target: Carbonic anhydrase (Enzyme)
UniProt: P40881 (CAH_METTE)
Organism: Methanosarcina thermophila
Activity: Ki = 6.39
Assay: Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila
Drug: dorzolamide
Target: Carbonic anhydrase (Enzyme)
UniProt: Q50565 (Q50565_METTH)
Organism: Methanothermobacter thermautotrophicus (strain ATCC 29096 / DSM 1053 / JCM 10044 / NBRC 100330 / Delta H)
Activity: Ki = 4.51
Assay: Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum
Drug: dorzolamide
Target: Carbonic anhydrase 13 (Enzyme)
Gene: CA13
UniProt: Q8N1Q1 (CAH13_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.74
Assay: Inhibition of human carbonic anhydrase13 preincubated for 15 mins by stopped-flow CO2 hydration assay
Drug: dorzolamide
Target: Carbonic anhydrase 15 (Enzyme)
Gene: Ca15
UniProt: Q99N23 (CAH15_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.21
Assay: Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay
Drug: dorzolamide
Target: Carbonic anhydrase (Enzyme)
Gene: NCE103
UniProt: P53615 (CAN_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 6.96
Assay: Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay
Drug: dorzolamide
Target: Carbonic anhydrase (Enzyme)
Gene: NCE103
UniProt: Q5AJ71 (CAN_CANAL)
Organism: Candida albicans (strain SC5314 / ATCC MYA-2876)
Activity: Ki = 8.05
Assay: Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay