AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: docosanoic acid
Target: Peroxisome proliferator-activated receptor delta (Nuclear hormone receptor)
Gene: PPARD
UniProt: Q03181 (PPARD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.52
Assay: Displacement of [3H]GW2433 from Homo sapiens (human) PPARdelta receptor by scintillation proximity assay
Drug: alitretinoin
Target: Retinoic acid receptor alpha (Nuclear hormone receptor)
Gene: RARA
UniProt: P10276 (RARA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.52
Action type: AGONIST
Drug: alitretinoin
Target: Retinoic acid receptor RXR-alpha (Nuclear hormone receptor)
Gene: RXRA
UniProt: P19793 (RXRA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.5
Action type: AGONIST
Drug: alitretinoin
Target: Retinoic acid receptor RXR-beta (Nuclear hormone receptor)
Gene: RXRB
UniProt: P28702 (RXRB_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.7
Action type: AGONIST
Drug: alitretinoin
Target: Retinoic acid receptor RXR-gamma (Nuclear hormone receptor)
Gene: RXRG
UniProt: P48443 (RXRG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.66
Action type: AGONIST
Drug: alitretinoin
Target: Retinoic acid receptor beta (Nuclear hormone receptor)
Gene: RARB
UniProt: P10826 (RARB_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.3
Action type: AGONIST
Drug: alitretinoin
Target: Retinoic acid receptor gamma (Nuclear hormone receptor)
Gene: RARG
UniProt: P13631 (RARG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.13
Action type: AGONIST
Drug: alitretinoin
Target: Nuclear receptor ROR-gamma (Nuclear hormone receptor)
Gene: RORC
UniProt: P51449 (RORG_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.85
Assay: Inverse agonist activity at human RoRc-LBD fusion protein with GST expressed in BL-21 (BL3) cells assessed as SRC1 coactivator peptide recruitment
Drug: alitretinoin
Target: Retinoic acid receptor RXR-beta (Transcription factor)
Gene: Rxrb
UniProt: P28704 (RXRB_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.92
Assay: Dissociation constant for binding to Retinoid X receptor beta
Drug: alitretinoin
Target: Retinoic acid receptor RXR-gamma (Transcription factor)
Gene: Rxrg
UniProt: P28705 (RXRG_MOUSE)
Organism: Mus musculus
Activity: Kd = 8.4
Assay: Dissociation constant for binding to Retinoid X receptor gamma
Drug: alitretinoin
Target: Retinoic acid receptor alpha (Transcription factor)
Gene: Rara
UniProt: P11416 (RARA_MOUSE)
Organism: Mus musculus
Activity: Kd = 8.15
Assay: Dissociation constant for binding to Retinoic acid receptor alpha
Drug: alitretinoin
Target: Retinoic acid receptor RXR-alpha (Transcription factor)
Gene: Rxra
UniProt: P28700 (RXRA_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.49
Assay: Dissociation constant for binding to Retinoid X receptor alpha
Drug: alitretinoin
Target: Retinoic acid receptor beta (Transcription factor)
Gene: Rarb
UniProt: P22605 (RARB_MOUSE)
Organism: Mus musculus
Activity: Kd = 8.15
Assay: Dissociation constant for binding to Retinoic acid receptor beta
Drug: alitretinoin
Target: Retinoic acid receptor gamma (Transcription factor)
Gene: Rarg
UniProt: P18911 (RARG_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.77
Assay: Dissociation constant for binding to Retinoic acid receptor gamma
Drug: alitretinoin
Target: Retinoic acid receptor RXR-alpha (Nuclear hormone receptor)
Gene: Rxra
UniProt: Q05343 (RXRA_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.96
Assay: Agonist activity at RXR-alpha in rat R3KE cells infected with oncogene KLF4-ER assessed as inhibition of KLF4-mediated oncogenic transformation
Drug: alitretinoin
Target: Nuclear receptor subfamily 4 group A member 1 (Nuclear other)
Gene: NR4A1
UniProt: P22736 (NR4A1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.09
Assay: Binding affinity to Nur77 Y453A mutant expressed in human BGC823 cells
Drug: alitretinoin
Target: Oxysterols receptor LXR-beta (Nuclear other)
Gene: NR1H2
UniProt: P55055 (NR1H2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.76
Assay: Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
Drug: alitretinoin
Target: Oxysterols receptor LXR-alpha (Nuclear other)
Gene: NR1H3
UniProt: Q13133 (NR1H3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.96
Assay: Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
Drug: artemisinin
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.699
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: benzamycin
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.41
Assay: Inhibition of human ERG expressed in HEK cells
Drug: benzamycin
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.01
Assay: Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis
Drug: benzamycin
Target: Motilin receptor (GPCR)
Gene: MLNR
UniProt: O43193 (MTLR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.36
Assay: Compound was tested for in vitro motilin receptor binding affinity
Drug: benzamycin
Target: Cytochrome P450 1B1 (Enzyme)
Gene: CYP1B1
UniProt: Q16678 (CP1B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.4
Assay: Inhibition of CYP1B1 (unknown origin) expressed in Escherichia coli DH5alpha coexpressing human NADPH-P450 reductase using 7-Ethoxyresorufin as substrate up to 6 mins in presence of NADP+ by spectrofluorometric analysis
Drug: benidipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.843
Action type: BLOCKER
Assay: HEK-293 cells stably expressing hCav3.2 T-type Ca2+ channels
Drug: benidipine
Target: Voltage-gated L-type calcium channel (Ion channel)
Gene: CACNA1D|CACNA1C
UniProt: Q01668|Q13936 (CAC1D_HUMAN|CAC1C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.31
Action type: BLOCKER
Assay: Inhibition of human L-type calcium channel Ca<sub>v</sub>1.2 in <i>Xenopus</i> oocyte, measured using 2-electrode voltage-clamp.
Drug: benzydamine
Target: Soluble guanylate cyclase (Enzyme)
Gene: GUCY1B2|GUCY1A2|GUCY1A3|GUCY1B3
UniProt: O75343|P33402|Q02108|Q02153 (GCYB2_HUMAN|GCYA2_HUMAN|GCYA3_HUMAN|GCYB1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.99
Assay: The cGMP produced by compound was expressed as a ratio between the percentage of the DEA/NO response for the compound
Drug: biriperone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.96
Assay: Ability to compete with [3H]YM-09151-2 binding to the human dopamine receptor D3 transfected in CHO cells
Drug: biriperone
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.88
Drug: biriperone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.62
Drug: biriperone
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.37
Drug: clobetasone butyrate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: clorotepine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.17
Assay: Displacement of [3H]prozosin from human cloned dopamine D2 receptor expressed in CHO cells
Drug: clorotepine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.24
Assay: Displacement of [3H]prozosin from human cloned 5HT2C receptor expressed in CHO cells
Drug: clorotepine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.665
Drug: clorotepine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.372
Drug: clorotepine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.72
Assay: Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
Drug: clorotepine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.398
Drug: clorotepine
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.307
Drug: clorotepine
Target: Potassium channel subfamily K member 9 (Ion channel)
Gene: KCNK9
UniProt: Q9NPC2 (KCNK9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.13
Assay: Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Drug: clorotepine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: Adra1d
UniProt: P23944 (ADA1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.11
Assay: Displacement of [3H]prozosin from rat cloned alpha1d receptor
Drug: clorotepine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.3
Assay: Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate
Drug: clorotepine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.64
Assay: Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate
Drug: clorotepine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.64
Assay: Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
Drug: clorotepine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.18
Assay: Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
Drug: clorotepine
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.62
Assay: Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate
Drug: clorotepine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P18841 (ADA1B_MESAU)
Organism: Mesocricetus auratus
Activity: Ki = 9.25
Assay: Displacement of [3H]prozosin from hamster cloned alpha-1b receptor
Drug: clorotepine
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 = 8.52
Assay: Ability to displace [3H]haloperidol from rat striatal membranes, in order to measure its intrinsic affinity for the dopamine (DA) receptor
Drug: clorotepine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.74
Assay: Ability to inhibit binding of [3H]PRAZ to alpha-1 adrenergic receptor in rat brain
Drug: clorotepine
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P08909|P14842|P30994 (5HT2C_RAT|5HT2A_RAT|5HT2B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.24
Assay: Ability to inhibit binding of [3H]KET to 5-hydroxytryptamine 2 receptor in rat cortex
Drug: dexamethasone phosphate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.3
Action type: AGONIST
Assay: Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 24 hrs
Drug: dexamethasone phosphate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.44
Assay: Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells
Drug: dexamethasone phosphate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells
Drug: dexamethasone phosphate
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.25
Assay: Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells
Drug: dexamethasone phosphate
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.79
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: dexamethasone phosphate
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.66
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
Drug: dexamethasone phosphate
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.52
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: dexamethasone phosphate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.66
Assay: Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting
Drug: androstanolone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.27
Assay: Binding affinity to GR (unknown origin)
Drug: androstanolone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.44
Assay: Binding affinity to MR (unknown origin)
Drug: androstanolone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Assay: Displacement of [3H]DHT from human androgen receptor expressed in MDA-MB-453 cells by whole cell receptor binding assay
Drug: androstanolone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.14
Assay: Binding affinity to PR (unknown origin)
Drug: androstanolone
Target: Aromatase (Enzyme)
Gene: CYP19A1
UniProt: P11511 (CP19A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.66
Assay: Competitive inhibition of binding to human placental Cytochrome P450 19A1
Drug: androstanolone
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.92
Drug: androstanolone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.74
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: androstanolone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.57
Assay: Binding affinity to rat androgen receptor by competitive inhibition assay
Drug: androstanolone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.788
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: androstanolone
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.7
Assay: Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting
Drug: androstanolone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P19091 (ANDR_MOUSE)
Organism: Mus musculus
Activity: IC50 = 9
Assay: Displacement of [3H] ]5alpha-DHT from mouse androgen receptor expressed in monkey COS7 cells after 2 hrs by scintillation counting analysis
Drug: androstanolone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: P06186 (PRGR_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 6.36
Assay: Displacement of [3H]progesterone from rabbit PR by liquid scintillation counting
Drug: androstanolone
Target: Mineralocorticoid receptor (Transcription factor)
Gene: Nr3c2
UniProt: P22199 (MCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.68
Assay: Displacement of [3H]aldosterone from Sprague-Dawley rat MR by liquid scintillation counting
Drug: dolasetron
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.226
Drug: dolasetron
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.698
Action type: ANTAGONIST
Drug: etoposide phosphate
Target: DNA topoisomerase 2-alpha (Enzyme)
Gene: TOP2A
UniProt: P11388 (TOP2A_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1806; SINGLE PROTEIN
Drug: guanabenz
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.824
Action type: AGONIST
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: guanabenz
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.928
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: guanabenz
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.951
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: guanabenz
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.208
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: guanabenz
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.971
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: guanabenz
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.167
Action type: AGONIST
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: guanabenz
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.793
Action type: AGONIST
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: guanabenz
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.801
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: guanabenz
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: MAOA
UniProt: P21397 (AOFA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.748
Assay: DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
Drug: guanabenz
Target: Trace amine-associated receptor 1 (GPCR)
Gene: TAAR1
UniProt: Q96RJ0 (TAAR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.05
Assay: Agonist activity at human TAAR1 receptor expressed in HEK293T cells cotransfected with beta-2 receptor assessed as cAMP production by BRET assay
Drug: guanabenz
Target: Nischarin (Membrane receptor)
Gene: NISCH
UniProt: Q9Y2I1 (NISCH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.46
Assay: Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
Drug: guanabenz
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.31
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: guanabenz
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.122
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: guanabenz
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.41
Drug: guanabenz
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.68
Drug: guanabenz
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 = 8.77
Assay: 50% inhibition of specific [3H]clonidine binding (0.4 nM) to Alpha-2 adrenergic receptors in rat isolated brain membranes
Drug: hydrocortisone butyrate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN
Drug: ilaprazole
Target: Potassium-transporting ATPase (Transporter)
Gene: ATP4A|ATP4B
UniProt: P20648|P51164 (ATP4A_HUMAN|ATP4B_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: ivermectin
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.646
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: ivermectin
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.66
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: ivermectin
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Drug: ivermectin
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.407
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: ivermectin
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.125
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: ivermectin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.924
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ivermectin
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.891
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ivermectin
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.586
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: ivermectin
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.244
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: ivermectin
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.451
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)