AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: clozapine
Target: Calmodulin-1 (Cytosolic other)
Gene: CALM1
UniProt: P0DP23 (CALM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.7
Assay: Binding affinity to CaM (unknown origin) by equilibrium dialysis method
Drug: cocaine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: cocaine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.05
Assay: Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand
Drug: cocaine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.14
Drug: cocaine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.92
Drug: cocaine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.57
Drug: cocaine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.68
Drug: cocaine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.67
Drug: cocaine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.47
Drug: cocaine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.5
Action type: INHIBITOR
Assay: Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (high affinity)
Drug: cocaine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.71
Drug: cocaine
Target: Sodium- and chloride-dependent GABA transporter 1 (Transporter)
Gene: SLC6A1
UniProt: P30531 (SC6A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.5
Drug: cocaine
Target: Sodium channel protein type 11 subunit alpha (Ion channel)
Gene: SCN11A
UniProt: Q9UI33 (SCNBA_HUMAN)
Organism: Homo sapiens
Drug: cocaine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Drug: cocaine
Target: Cocaine- and amphetamine-regulated transcript protein (Transcription factor)
Gene: CARTPT
UniProt: Q16568 (CART_HUMAN)
Organism: Homo sapiens
Drug: cocaine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.21
Assay: Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 of rat brain membrane
Drug: cocaine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: P31652 (SC6A4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.35
Assay: Binding affinity towards serotonin transporter 5-HTT was determined using [3H]paroxetine radioligand.
Drug: cocaine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.49
Assay: Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen
Drug: cocaine
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.97
Assay: Inhibition of high affinity uptake of [3H]NE by norepinephrine transporter in nerve endings obtained from rat brain.
Drug: cocaine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: Q61327 (SC6A3_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.7
Assay: Inhibition of mouse DAT expressed in HEK293 cells assessed as reduction in [3H]-DA uptake
Drug: cocaine
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.5
Assay: Displacement of [3H]nisoxetine from NET in rat brain
Drug: cocaine
Target: Serotonin 3 receptor (5HT3) (Ion channel)
Gene: HTR3B|HTR3A
UniProt: O95264|P46098 (5HT3B_HUMAN|5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.8
Action type: ANTAGONIST
Drug: cocaine
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 = 4.31
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: cocaine
Target: Dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: P27922 (SC6A3_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.19
Assay: In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue
Drug: cocaine
Target: Dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q9GJT6 (SC6A3_MACFA)
Organism: Macaca fascicularis
Activity: IC50 = 7.02
Assay: Inhibition of [3H]WIN-35428 binding to dopamine transporter (DAT) of cynomolgus monkey caudate-putamen
Drug: codeine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.14
Action type: AGONIST
Assay: Displacement of [3H]diprenorphine from recombinant mu opioid receptor expressed in C6 cells
Drug: codeine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.59
Action type: AGONIST
Assay: Displacement of [3H]diprenorphine from recombinant kappa opioid receptor expressed in CHO cells
Drug: codeine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.28
Action type: AGONIST
Assay: Displacement of [3H]diprenorphine from recombinant delta opioid receptor expressed in C6 cells
Drug: codeine
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 = 8
Assay: 50% Inhibition of stereospecific [3H]-naltrexone (10e-9 M) binding towards opiate receptor in rat brain homogenate
Drug: colchicine
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.19
Drug: colchicine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 3.801
Drug: colchicine
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Drug: colchicine
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.49
Drug: colchicine
Target: Glycine receptor subunit alpha-2 (Ion channel)
Gene: GLRA2
UniProt: P23416 (GLRA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.194
Drug: colchicine
Target: Tubulin beta chain (Structural)
Gene: TUBB
UniProt: P07437 (TBB5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.24
Action type: INHIBITOR
Drug: colchicine
Target: Serine/threonine-protein kinase pim-1 (Kinase)
Gene: PIM1
UniProt: P11309 (PIM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.37
Assay: Inhibition of human PIM1 measured after 5 mins by ELISA relative to control
Drug: colchicine
Target: Tubulin alpha-1A chain (Structural)
Gene: TUBA1A
UniProt: P02550 (TBA1A_PIG)
Organism: Sus scrofa
Activity: Ki = 5.6
Assay: Compound was evaluated for its ability to inhibit the binding of [3H]-colchicine to tubulin in competitive binding assay
Drug: colchicine
Target: Tubulin beta-2B chain (Structural)
Gene: TUBB2B
UniProt: Q6B856 (TBB2B_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.11
Assay: Binding constant at colchicine site of bovine brain tubulin
Drug: colchicine
Target: Bromodomain-containing protein 4 (Unclassified)
Gene: BRD4
UniProt: O60885 (BRD4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.7
Action type: INHIBITOR
Drug: colchicine
Target: Tubulin polymerization-promoting protein (Unclassified)
Gene: TPPP
UniProt: Q27957 (TPPP_BOVIN)
Organism: Bos taurus
Activity: EC50 = 6.12
Assay: Inhibition of Bos taurus (bovine) brain tubulin polymerization
Drug: colchicine
Target: Tubulin beta-4B chain (Structural)
Gene: TUBB4B
UniProt: P68371 (TBB4B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.24
Drug: colchicine
Target: Tubulin (Structural)
Gene: TUBB2B
UniProt: Q6B856|Q862F3|Q862L2 (TBB2B_BOVIN|Q862F3_BOVIN|Q862L2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.1
Assay: Inhibition of bovine brain tubulin polymerization (ITP).
Drug: colchicine
Target: Tubulin (Structural)
Gene: TUBA1A
UniProt: P02550|P02554 (TBA1A_PIG|TBB_PIG)
Organism: Sus scrofa
Activity: Ki = 5.24
Assay: Binding affinity against tubulin usingf [3H]-colchicine as radioligand
Drug: colforsin daropate
Target: Adenylate cyclase type 1 (Enzyme)
Gene: ADCY1
UniProt: Q08828 (ADCY1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.39
Assay: Inhibition of [125 I]6-IHPP-forskolin binding to adenylate cyclase 1
Drug: colforsin daropate
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 = 4.22
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: colforsin daropate
Target: Solute carrier family 2, facilitated glucose transporter member 1 (Transporter)
Gene: SLC2A1
UniProt: P11166 (GTR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.3
Assay: Inhibition of [125I]7-IHPP-Fsk binding to glucose transporter of human erythrocyte membrane
Drug: colforsin daropate
Target: Adenylate cyclase type 1 (Enzyme)
Gene: ADCY1
UniProt: P19754 (ADCY1_BOVIN)
Organism: Bos taurus
Activity: Kd = 7.54
Drug: conivaptan
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.37
Action type: ANTAGONIST
Assay: Displacement [3H]Arg human recombinant Vasopressin V1a receptor
Drug: conivaptan
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.44
Action type: ANTAGONIST
Assay: Displacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug: conivaptan
Target: Oxytocin receptor (GPCR)
Gene: Oxtr
UniProt: P70536 (OXYR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.35
Assay: Displacement of [3H]OT from OTR in Wistar rat uterus membranes incubated for 60 mins by microplate scintillation counting method
Drug: conivaptan
Target: Vasopressin V2 receptor (GPCR)
Gene: Avpr2
UniProt: Q00788 (V2R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.52
Assay: Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug: conivaptan
Target: Vasopressin V1a receptor (GPCR)
Gene: Avpr1a
UniProt: P30560 (V1AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.32
Assay: Displacement of [3H]AVP from V1A receptor in Wistar rat liver membranes incubated for 60 mins by microplate scintillation counting method
Drug: cortisone acetate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.02
Action type: AGONIST
Drug: cortisone acetate
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: cortisone acetate
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.89
Drug: cortisone acetate
Target: Potassium voltage-gated channel subfamily A member 1 (Ion channel)
Gene: KCNA1
UniProt: Q09470 (KCNA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.48
Assay: Activation of KV1.1 expressed in Xenopus laevis oocytes coexpressing Kvbeta1 W155A mutant assessed as increase in steady state current normalized to initial inactivating current by electrophysiology method
Drug: cortisone acetate
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.43
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: cortisone acetate
Target: Multidrug and toxin extrusion protein 1 (Transporter)
Gene: SLC47A1
UniProt: Q96FL8 (S47A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.67
Assay: Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Drug: cortisone acetate
Target: Protein farnesyltransferase (Enzyme)
Gene: FNTA|FNTB
UniProt: P49354|P49356 (FNTA_HUMAN|FNTB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.85
Assay: inhibitory activity against human Farnesyltransferase
Drug: cortivazol
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: cotinine
Target: Neuronal acetylcholine receptor subunit alpha-2 (Ion channel)
Gene: CHRNA2
UniProt: Q15822 (ACHA2_HUMAN)
Organism: Homo sapiens
Drug: coumarin
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.04
Assay: Inhibition of full length human CA2 cytosolic isoform by stopped-flow CO2 hydration method
Drug: coumarin
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.51
Assay: Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.17
Assay: Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.04
Assay: Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.05
Assay: Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.03
Assay: Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.28
Assay: Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.48
Assay: Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 3 (Enzyme)
Gene: CA3
UniProt: P07451 (CAH3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.25
Assay: Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 6 (Enzyme)
Gene: CA6
UniProt: P23280 (CAH6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.7
Assay: Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.32
Assay: Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Carbonic anhydrase 13 (Enzyme)
Gene: Ca13
UniProt: Q9D6N1 (CAH13_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.04
Assay: Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration assay
Drug: coumarin
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: Maob
UniProt: P19643 (AOFB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.92
Assay: Inhibitory effect on Monoamine oxidase B, SD on IC50 values < 10%
Drug: coumarin
Target: Amine oxidase [flavin-containing] A (Enzyme)
Gene: Maoa
UniProt: P21396 (AOFA_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.39
Assay: Inhibitory effect on monoamine oxidase A, SD on IC50 values < 10%
Drug: coumarin
Target: Carbonic anhydrase 15 (Enzyme)
Gene: Ca15
UniProt: Q99N23 (CAH15_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.4
Assay: Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration assay
Drug: cromoglicic acid
Target: G protein-coupled receptor GPR35 (GPCR)
Gene: Gpr35
UniProt: Q33BM1 (Q33BM1_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 6.01
Assay: Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Drug: cromoglicic acid
Target: G-protein coupled receptor 35 (GPCR)
Gene: Gpr35
UniProt: Q9ES90 (GPR35_MOUSE)
Organism: Mus musculus
Activity: EC50 = 5.32
Assay: Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Drug: cromoglicic acid
Target: G-protein coupled receptor 35 (GPCR)
Gene: GPR35
UniProt: Q9HC97 (GPR35_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.63
Assay: Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis
Drug: cromoglicic acid
Target: Protein S100-P (Cytosolic other)
Gene: S100P
UniProt: P25815 (S100P_HUMAN)
Organism: Homo sapiens
Assay: cromolyn blocked the coimmunoprecipitation of S100P and RAGE
Drug: cyamemazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.42
Drug: cyamemazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.237
Drug: cyamemazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Action type: ANTAGONIST
Drug: cyamemazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.8
Action type: ANTAGONIST
Drug: cyamemazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Action type: ANTAGONIST
Drug: cyamemazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: cyamemazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.602
Drug: cyamemazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.886
Drug: cyamemazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.377
Drug: cyamemazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.495
Drug: cyamemazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.921
Drug: cyamemazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.456
Drug: cyamemazine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.531
Drug: cyclizine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.235
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: cyclizine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.194
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: cyclizine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.623
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: cyclizine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.272
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: cyclizine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.993
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: cyclizine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.353
Action type: ANTAGONIST
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: cyclizine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.788
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyclizine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.385
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyclizine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.799
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyclizine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.924
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyclizine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.342
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyclizine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.218
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: cyclizine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.206
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: cyclizine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.224
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cyclizine
Target: Amine oxidase [flavin-containing] B (Enzyme)
Gene: MAOB
UniProt: P27338 (AOFB_HUMAN)
Organism: Homo sapiens
Drug: cyclizine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.86
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cyclobenzaprine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.728
Drug: cyclobenzaprine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.967
Drug: cyclobenzaprine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.444
Drug: cyclobenzaprine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.541
Action type: ANTAGONIST