AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: chloroquine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.48
Assay: Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
Drug: chloroquine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.24
Assay: Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4)  by displacement of 3H-QNB
Drug: chloroquine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.66
Assay: Activity of compound against Muscarinic acetylcholine receptor M5 (CHRM5) by displacement of 3H-QNB
Drug: chloroquine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Assay: Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine
Drug: chloroquine
Target: Ribosyldihydronicotinamide dehydrogenase [quinone] (Enzyme)
Gene: NQO2
UniProt: P16083 (NQO2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.82
Assay: Inhibition of human recombinant NQO2
Drug: chloroquine
Target: Beta-secretase 1 (Enzyme)
Gene: BACE1
UniProt: P56817 (BACE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.16
Assay: Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 40) level after 24 hrs by ELISA method
Drug: chloroquine
Target: Major prion protein (Surface antigen)
Gene: PRNP
UniProt: P04156 (PRIO_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.4
Assay: Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
Drug: chloroquine
Target: Histidine-rich protein PFHRP-II (Cytosolic other)
UniProt: P05227 (HRP1_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 6.4
Assay: Inhibition of beta-hematin polymerization
Drug: chloroquine
Target: Riboflavin-binding protein (Unclassified)
UniProt: P02752 (RBP_CHICK)
Organism: Gallus gallus
Activity: Kd = 5.68
Assay: Binding affinity to chicken riboflavin binding protein assessed as dissociation constant at pH 7.4 in phosphate buffer by isothermal titration calorimetric assay
Drug: chloroquine
Target: Dihydrofolate reductase (Enzyme)
Gene: DHFR
UniProt: P00376 (DYR_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.52
Assay: Inhibition of bovine liver DHFR
Drug: chloroquine
Target: Amyloid beta A4 protein (Unclassified)
Gene: APP
UniProt: P05067 (A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.16
Assay: Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 40 residues) production measured after 24 hrs
Drug: chloroquine
Target: Transmembrane protein 97 (Enzyme)
Gene: TMEM97
UniProt: Q5BJF2 (TMM97_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Assay: Displacement of [3H]-DTG from the Sigma2 receptor
Drug: chloroquine
Target: Cysteine proteinase falcipain 2a (Enzyme)
UniProt: Q9N6S8 (Q9N6S8_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 7.7
Assay: Inhibition of falcipain-2 in chloroquine sensitive Plasmodium falciparum MRC-02 schizont stage infected in human erythrocytes assessed as reduction in bacterial growth after 24 hrs by Giemsa staining based assay
Drug: chlorothiazide
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Drug: chlorothiazide
Target: Solute carrier family 12 member 3 (Transporter)
Gene: SLC12A3
UniProt: P55017 (S12A3_HUMAN)
Organism: Homo sapiens
Activity: A2 = 5.43
Action type: INHIBITOR
Drug: chlorotrianisene
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Drug: chlorotrianisene
Target: Estrogen receptor beta (Nuclear hormone receptor)
Gene: ESR2
UniProt: Q92731 (ESR2_HUMAN)
Organism: Homo sapiens
Action type: MODULATOR
Assay: Mechanism of Action; CHEMBL242; SINGLE PROTEIN
Drug: chloroxine
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: ALOX5
UniProt: P09917 (LOX5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.44
Assay: Inhibition of human 5-lipoxygenase assessed as conjugated diene product formation using arachidonic acid by UV-vis spectrophotometer analysis
Drug: chloroxine
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P16050 (LOX15_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.62
Assay: Inhibition of human reticulocyte N-terminally His6-tagged 15-lipoxygenase-1 assessed as conjugated diene product formation using arachidonic acid by UV-vis spectrophotometer analysis
Drug: chloroxine
Target: Arachidonate 12-lipoxygenase, 12S-type (Enzyme)
Gene: ALOX12
UniProt: P18054 (LOX12_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.72
Assay: Inhibition of human platelet-type N-terminally His6-tagged 12-lipoxygenase assessed as conjugated diene product formation using arachidonic acid by UV-vis spectrophotometer analysis
Drug: chloroxine
Target: Botulinum neurotoxin type A (Enzyme)
Gene: botA
UniProt: P10845 (BXA1_CLOBO)
Organism: Clostridium botulinum
Activity: IC50 = 4.94
Assay: Inhibition of Clostridium botulinum BoNT/A LC expressed in Escherichia coli assessed as cleavage of SNAPtide preincubated for 5 mins followed by SNAPtide addition measured for 105 mins by fluorescence assay
Drug: chloroxine
Target: Arachidonate 15-lipoxygenase, type II (Enzyme)
Gene: ALOX15B
UniProt: O15296 (LX15B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.55
Assay: Inhibition of human reticulocyte N-terminally His6-tagged 15-lipoxygenase-2 assessed as conjugated diene product formation using arachidonic acid by UV-vis spectrophotometer analysis
Drug: chlorphenamine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Inhibitory concentration against IKr potassium channel
Drug: chlorphenamine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.818
Drug: chlorphenamine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.167
Drug: chlorphenamine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.15
Action type: ANTAGONIST
Drug: chlorphenamine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.67
Drug: chlorphenamine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.967
Drug: chlorphenamine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 8.06
Assay: Inhibition of [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex
Drug: chlorphenamine
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Assay: Ability to displace [3H]pyrilamine from histamine H1 receptor in male Sprague-Dawley rat brain membranes
Drug: chlorphenamine
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 = 5
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: chlorphenamine
Target: Lethal(3)malignant brain tumor-like protein 1 (Unclassified)
Gene: L3MBTL1
UniProt: Q9Y468 (LMBL1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.39
Assay: Inhibition of L3MBTL1 by alpha-screening
Drug: chlorphenamine
Target: Lethal(3)malignant brain tumor-like protein 3 (Unclassified)
Gene: L3MBTL3
UniProt: Q96JM7 (LMBL3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.38
Assay: Inhibition of L3MBTL3 by alpha-screening
Drug: chlorphenamine
Target: MBT domain-containing protein 1 (Unclassified)
Gene: MBTD1
UniProt: Q05BQ5 (MBTD1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.47
Assay: Inhibition of MBTD1 by alpha-screening
Drug: chlorphenamine
Target: Chloroquine resistance transporter (Transporter)
Gene: CRT
UniProt: Q9N623 (CRT_PLAFA)
Organism: Plasmodium falciparum
Activity: IC50 = 4.27
Assay: Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs
Drug: chlorphenamine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.842
Drug: chlorphenamine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.975
Drug: chlorphentermine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.471
Action type: SUBSTRATE
Drug: chlorphentermine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.404
Drug: chlorproethazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.979
Drug: chlorproethazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.987
Drug: chlorproethazine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.638
Drug: chlorpromazine
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.233
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: chlorpromazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.19
Drug: chlorpromazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.15
Action type: ANTAGONIST
Drug: chlorpromazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.2
Drug: chlorpromazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.724
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: chlorpromazine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.83
Drug: chlorpromazine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Assay: High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model
Drug: chlorpromazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.92
Assay: Binding affinity to SERT (unknown origin) by radioligand binding assay
Drug: chlorpromazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.721
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.17
Assay: Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in cloned CHO cells
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Action type: ANTAGONIST
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.28
Assay: Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.44
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.41
Drug: chlorpromazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  9.553
Drug: chlorpromazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Drug: chlorpromazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.54
Action type: ANTAGONIST
Drug: chlorpromazine
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.93
Drug: chlorpromazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Drug: chlorpromazine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.759
Drug: chlorpromazine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.87
Drug: chlorpromazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.602
Drug: chlorpromazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.746
Drug: chlorpromazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.251
Drug: chlorpromazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.398
Drug: chlorpromazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.377
Drug: chlorpromazine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.244
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.827
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.345
Drug: chlorpromazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Drug: chlorpromazine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.678
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: chlorpromazine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.155
Drug: chlorpromazine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.69
Action type: ANTAGONIST
Drug: chlorpromazine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.708
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.01
Drug: chlorpromazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.092
Drug: chlorpromazine
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.353
Assay: DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: chlorpromazine
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.91
Assay: Binding affinity to human calmodulin expressed in Escherichia coli using M124C-mBBr fluorescent biosensor by spectrofluorometer analysis
Drug: chlorpromazine
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.133
Assay: DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.928
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.463
Drug: chlorpromazine
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.54
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: chlorpromazine
Target: Potassium channel subfamily K member 2 (Ion channel)
Gene: KCNK2
UniProt: O95069 (KCNK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.57
Assay: Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents
Drug: chlorpromazine
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.061
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: chlorpromazine
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.713
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: chlorpromazine
Target: Ryanodine receptor 1 (Ion channel)
Gene: RYR1
UniProt: P21817 (RYR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.569
Drug: chlorpromazine
Target: Major prion protein (Surface antigen)
Gene: PRNP
UniProt: P04156 (PRIO_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.7
Assay: Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
Drug: chlorpromazine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.57
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: chlorpromazine
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.043
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: chlorpromazine
Target: Trypanothione reductase (Enzyme)
Gene: TPR
UniProt: P28593 (TYTR_TRYCR)
Organism: Trypanosoma cruzi
Activity: Ki = 5.49
Assay: Inhibition of Trypanosoma cruzi recombinant trypanothione reductase
Drug: chlorpromazine
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 4.797
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: chlorpromazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.305
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.736
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: chlorpromazine
Target: Melanocortin receptor 4 (GPCR)
Gene: MC4R
UniProt: P32245 (MC4R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.835
Assay: DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: chlorpromazine
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.146
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: chlorpromazine
Target: Melanocortin receptor 3 (GPCR)
Gene: MC3R
UniProt: P41968 (MC3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.673
Assay: DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: chlorpromazine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.777
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: chlorpromazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.07
Drug: chlorpromazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.3
Drug: chlorpromazine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.92
Assay: Compound was tested for inhibitory activity against the binding of [3H]spiperone to Dopamine receptor D2 in rat striatal membranes
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.75
Assay: The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.68
Assay: Binding affinity towards rat 5-hydroxytryptamine 7 receptor
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.3
Action type: ANTAGONIST
Drug: chlorpromazine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.46
Assay: In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug: chlorpromazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: IC50 = 7.1
Assay: Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes.
Drug: chlorpromazine
Target: Transient receptor potential cation channel subfamily V member 1 (Ion channel)
Gene: Trpv1
UniProt: O35433 (TRPV1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.89
Assay: Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells
Drug: chlorpromazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.4
Action type: ANTAGONIST
Drug: chlorpromazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 5.35
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: chlorpromazine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.854