AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: clotrimazole
Target: C-X-C chemokine receptor type 1 (GPCR)
Gene: CXCR1
UniProt: P25024 (CXCR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.7
Assay: Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug: clotrimazole
Target: 14-alpha sterol demethylase Cyp51A (Enzyme)
UniProt: Q4WNT5 (Q4WNT5_ASPFU)
Organism: Neosartorya fumigata (strain ATCC MYA-4609 / Af293 / CBS 101355 / FGSC A1100)
Activity: Kd = 5.32
Assay: Binding affinity to Aspergillus fumigatus AF293 sterol 14-alpha demethylase isoenzyme A expressed in Escherichia coli
Drug: clotrimazole
Target: 14-alpha sterol demethylase (Enzyme)
Gene: cyp51B
UniProt: Q96W81 (Q96W81_ASPFM)
Organism: Neosartorya fumigata
Activity: Kd = 6.99
Assay: Binding affinity to Aspergillus fumigatus AF293 sterol 14-alpha demethylase isoenzyme B expressed in Escherichia coli assessed as tight binding affinity constant
Drug: clotrimazole
Target: Indoleamine 2,3-dioxygenase 2 (Enzyme)
Gene: Ido2
UniProt: Q8R0V5 (I23O2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.23
Assay: Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: clotrimazole
Target: Mycocyclosin synthase (Enzyme)
Gene: cyp121
UniProt: P9WPP7 (CP121_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 7.14
Assay: Binding affinity to Mycobacterium tuberculosis H37Rv wild type CYP121 by titration assay
Drug: clotrimazole
Target: Transitional endoplasmic reticulum ATPase (Enzyme)
Gene: VCP
UniProt: P55072 (TERA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.85
Assay: Inhibition of p97 in human HeLa cells assessed as reduction in p97-dependent UbG76V-GFP degradation incubated for 1 hr by luciferase reporter gene assay
Drug: clotrimazole
Target: Malate dehydrogenase cytoplasmic  (Enzyme)
Gene: MDH1
UniProt: P40925 (MDHC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.46
Assay: Inhibition of malate dehydrogenase (MDH)
Drug: clotrimazole
Target: Putative cytochrome P450 130 (Enzyme)
Gene: cyp130
UniProt: P9WPN5 (CP130_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Kd = 4.88
Assay: Binding affinity to Mycobacterium tuberculosis CYP130
Drug: clotrimazole
Target: Alpha-chymotrypsin (Enzyme)
UniProt: P00766 (CTRA_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.07
Assay: Compound was tested for the inhibition of Chymotrypsinogen
Drug: clotrimazole
Target: Indoleamine 2,3-dioxygenase 1 (Enzyme)
Gene: Ido1
UniProt: P28776 (I23O1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.29
Assay: Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: clotrimazole
Target: 7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase (Enzyme)
Gene: CYP8B1
UniProt: Q9UNU6 (CP8B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.1
Assay: Inhibition of CYP8B1 in human liver microsomes using D7-7alpha-hydroxy-4-cholesten-3-one as substrate preincubated for 20 mins followed by substrate addition in presence of NADPH by UPLC-ESI-MS/MS analysis
Drug: cloxacillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: cloxacillin
Target: Beta-lactamase TEM (Enzyme)
Gene: bla; blaT-3; blaT-4;
UniProt: P62593 (BLAT_ECOLX)
Organism: Escherichia coli
Activity: Ki = 4.89
Assay: Inhibition constant (Ki) for TEM-1 beta-lactamase
Drug: cloxacillin
Target: Beta-lactamase (Enzyme)
Gene: blaACC-4
UniProt: A4ZYU9 (A4ZYU9_ECOLX)
Organism: Escherichia coli
Activity: IC50 = 7.59
Assay: Inhibition of Escherichia coli beta-lactamase ACC4
Drug: cloxacillin
Target: Efflux transporter; SugE (Transporter)
Gene: sugE
UniProt: Q3S5C3 (Q3S5C3_SALNE)
Organism: Salmonella newport
Activity: IC50 = 8.4
Assay: Inhibition of Salmonella enterica serotype Newport AM17274 cephalosporinase CMY-31 by UV spectrophotometer in presence of 100 uM of cephalothin
Drug: cloxacillin
Target: Beta-lactamase (Enzyme)
Gene: bla LAT-2
UniProt: Q48435 (Q48435_KLEPN)
Organism: Klebsiella pneumoniae
Activity: IC50 = 8.4
Assay: Inhibition of Klebsiella pneumoniae HP205 cephalosporinase CMY-36 by UV spectrophotometer in presence of 100 uM of cephalothin
Drug: cloxacillin
Target: Beta-lactamase TEM (Enzyme)
Gene: bla
UniProt: P62594 (BLAT_SALTI)
Organism: Salmonella typhi
Activity: Ki = 4.89
Drug: cloxacillin
Target: Penicillin-binding protein (Enzyme)
Gene: pbp4|mecA|pbpA|PBP2|pbpF
UniProt: P72355|Q53707|Q53725|Q53729|Q9XDB3 (P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU)
Organism: Staphylococcus aureus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2363021; PROTEIN FAMILY
Drug: cloxazolam
Target: Aldo-keto reductase family 1 member C3 (Enzyme)
Gene: AKR1C3
UniProt: P42330 (AK1C3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.82
Assay: Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90) (
Drug: clozapine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: clozapine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.783
Drug: clozapine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.89
Drug: clozapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.86
Action type: ANTAGONIST
Drug: clozapine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.154
Drug: clozapine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.2
Drug: clozapine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.6
Drug: clozapine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.41
Assay: Binding affinity to human SERT
Drug: clozapine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.83
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Assay: Binding affinity to 5-HT1A receptor (unknown origin)
Drug: clozapine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: ANTAGONIST
Drug: clozapine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Drug: clozapine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.05
Drug: clozapine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.95
Drug: clozapine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.78
Drug: clozapine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Drug: clozapine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.42
Drug: clozapine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.59
Action type: ANTAGONIST
Drug: clozapine
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.594
Drug: clozapine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.2
Drug: clozapine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.815
Drug: clozapine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.23
Drug: clozapine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.181
Drug: clozapine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Drug: clozapine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.591
Drug: clozapine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.222
Drug: clozapine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.792
Drug: clozapine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.356
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.2
Action type: AGONIST
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: AGONIST
Drug: clozapine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.54
Drug: clozapine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.81
Assay: Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Drug: clozapine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.52
Action type: ANTAGONIST
Drug: clozapine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.7
Action type: ANTAGONIST
Drug: clozapine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.28
Drug: clozapine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.98
Drug: clozapine
Target: UDP-glucuronosyltransferase 1-4 (Enzyme)
Gene: UGT1A4
UniProt: P22310 (UD14_HUMAN)
Organism: Homo sapiens
Activity: app Km = 4.208
Drug: clozapine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Assay: Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: AGONIST
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: AGONIST
Drug: clozapine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.445
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.6
Assay: Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug: clozapine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.66
Assay: Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
Drug: clozapine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 8.42
Assay: Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
Drug: clozapine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.34
Assay: Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by Radio ligand [3H]quinuclidinyl binding assay.
Drug: clozapine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.68
Assay: Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by radioligand [3H]pirenzepine binding assay.
Drug: clozapine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.47
Assay: In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.41
Assay: The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus
Drug: clozapine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.22
Assay: Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membrane
Drug: clozapine
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.16
Assay: Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter
Drug: clozapine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.2
Assay: Binding affinity towards rat 5-hydroxytryptamine 7 receptor
Drug: clozapine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.4
Action type: ANTAGONIST
Drug: clozapine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: Q95136 (DRD1_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.38
Assay: Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug: clozapine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P18090 (ADRB1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.59
Assay: Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug: clozapine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.37
Assay: Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug: clozapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P20288 (DRD2_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.16
Assay: Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2
Drug: clozapine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: Adra2a
UniProt: P22909 (ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.72
Assay: Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
Drug: clozapine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61168 (DRD2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.54
Assay: Inhibition of mouse Dopamine receptor D2
Drug: clozapine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.1
Assay: Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2C receptor
Drug: clozapine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: Q64264 (5HT1A_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.7
Assay: Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice.
Drug: clozapine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.8
Assay: Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin
Drug: clozapine
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.54
Assay: In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
Drug: clozapine
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.79
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: clozapine
Target: D(4) dopamine receptor (GPCR)
Gene: Drd4
UniProt: P30729 (DRD4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.05
Assay: Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug: clozapine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P52702 (DRD2_CHLAE)
Organism: Chlorocebus aethiops
Activity: Ki = 6.6
Assay: Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2
Drug: clozapine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: Q75Z89 (5HT2A_BOVIN)
Organism: Bos taurus
Activity: IC50 = 8.52
Assay: Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin
Drug: clozapine
Target: Histamine H3 receptor (GPCR)
Gene: Hrh3
UniProt: Q9QYN8 (HRH3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.8
Action type: ANTAGONIST
Drug: clozapine
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: Htr3a
UniProt: P23979 (5HT3A_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.49
Assay: Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay.
Drug: clozapine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.4
Action type: ANTAGONIST
Drug: clozapine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P50130 (DRD1_PIG)
Organism: Sus scrofa
Activity: Ki = 6.38
Assay: Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug: clozapine
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.41
Assay: Binding affinity to rat NET
Drug: clozapine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P52703 (DRD3_CHLAE)
Organism: Chlorocebus aethiops
Activity: Ki = 6.33
Assay: Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3
Drug: clozapine
Target: Histamine H4 receptor (GPCR)
Gene: Hrh4
UniProt: Q91ZY2 (HRH4_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.5
Action type: ANTAGONIST
Drug: clozapine
Target: Histamine H4 receptor (GPCR)
Gene: Hrh4
UniProt: Q91ZY1 (HRH4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.7
Action type: ANTAGONIST
Drug: clozapine
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: Htr3a|Htr3b
UniProt: P35563|Q9JJ16 (5HT3A_RAT|5HT3B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.28
Assay: Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 3 receptor
Drug: clozapine
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm3|Chrm4|Chrm5|Chrm2
UniProt: P08482|P08483|P08485|P08911|P10980 (ACM1_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT|ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.6
Assay: In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
Drug: clozapine
Target: Serotonin 1 (5-HT1) receptor (GPCR)
Gene: Htr1a|Htr1b|Htr1d|Htr1f
UniProt: P19327|P28564|P28565|P30940 (5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.68
Assay: The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue
Drug: clozapine
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 affinity towards alpha-2 adrenergic receptors in rat brain synaptosomal preparations
Drug: clozapine
Target: Dopamine receptor (GPCR)
Gene: DRD2|DRD1
UniProt: P20288|Q95136 (DRD2_BOVIN|DRD1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.74
Assay: Inhibition of [3H]haloperidol binding to Dopamine receptor in calf caudate nuclei.
Drug: clozapine
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: Ki = 6.49
Assay: In vitro ability to displace [3H]spiroperidol from rat dopamine receptor
Drug: clozapine
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: Ki = 8.74
Assay: Binding affinity determined in radioreceptor binding assay by using [3H]ketanserin radioligand against 5-hydroxytryptamine 2 receptor
Drug: clozapine
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: IC50 = 6.85
Assay: Inhibition of dopamine-sensitive rat brain adenylyl cyclase activity assessed as cAMP level
Drug: clozapine
Target: Serotonin 2 (5-HT2) receptor (GPCR)
Gene: Htr2c|Htr2a|Htr2b
UniProt: P34968|P35363|Q02152 (5HT2C_MOUSE|5HT2A_MOUSE|5HT2B_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.55
Assay: Inhibitory activity against serotonin 5-hydroxytryptamine 2 receptor from mice.
Drug: clozapine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: Htr5a
UniProt: P30966 (5HT5A_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.3
Action type: ANTAGONIST
Drug: clozapine
Target: Histone H1.0 (Nuclear other)
Gene: H1F0
UniProt: P07305 (H10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Assay: Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
Drug: clozapine
Target: Calmodulin (Cytosolic other)
Gene: CALM
UniProt: P62157 (CALM_BOVIN)
Organism: Bos taurus
Activity: Kd = 4.21
Assay: Binding affinity to bovine brain CaM by FTPFACE analysis