AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: progesterone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.07
Assay: Displacement of DHT from human androgen receptor expressed in baculovirus SF-12 cells
Drug: progesterone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: ED50 = 9.876
Action type: AGONIST
Drug: progesterone
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.38
Drug: progesterone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.94
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: progesterone
Target: Sterol O-acyltransferase 1 (Enzyme)
Gene: SOAT1
UniProt: P35610 (SOAT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.77
Assay: In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase
Drug: progesterone
Target: Fatty acid-binding protein, intestinal (Cytosolic other)
Gene: FABP2
UniProt: P12104 (FABPI_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.7
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP
Drug: progesterone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.81
Assay: Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
Drug: progesterone
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.57
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: progesterone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.441
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: progesterone
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: Q9R0C9 (SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Kd = 6.62
Assay: Displacement of [3H]pentazocine from sigma-1 opioid receptor in rat liver membranes after 1 hr by liquid scintillation spectrometric analysis
Drug: progesterone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P19091 (ANDR_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.43
Assay: Inhibitory activity against Androgen receptor
Drug: progesterone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: P06186 (PRGR_RABIT)
Organism: Oryctolagus cuniculus
Activity: Ki = 7.98
Assay: Inhibition of [3H]R5020 binding to rabbit uterine progesterone receptor
Drug: progesterone
Target: C-8 sterol isomerase (Enzyme)
Gene: ERG2
UniProt: P32352 (ERG2_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: Ki = 5.35
Assay: Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: progesterone
Target: Sigma non-opioid intracellular receptor 1 (Membrane other)
Gene: SIGMAR1
UniProt: Q60492 (SGMR1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.18
Assay: Displacement of (+)-[3H]pentazocine from guinea pig brain sigma 1 receptor after 180 mins by scintillation counting
Drug: progesterone
Target: Steroid 5-alpha-reductase (Enzyme)
Gene: Srd5a1|Srd5a2
UniProt: P24008|P31214 (S5A1_RAT|S5A2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.8
Assay: Inhibition of rat testosterone-5 alpha-reductase activity at pH 6.6 from rat
Drug: progesterone
Target: Estrogen receptor (Transcription factor)
Gene: Esr1|Esr2
UniProt: P06211|Q62986 (ESR1_RAT|ESR2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 8.41
Assay: Equilibrium dissociation constant for rat uterine estrogen receptor binding [3H]estradiol
Drug: progesterone
Target: Cation channel sperm-associated protein 1 (Ion channel)
Gene: CATSPER1
UniProt: Q8NEC5 (CTSR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.11
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluorometry,  2-3  &micro;M shows the saturating efficacy.
Drug: progesterone
Target: Cation channel sperm-associated protein 2 (Ion channel)
Gene: CATSPER2
UniProt: Q96P56 (CTSR2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.11
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluorometry; 2-3  &micro;M shows the saturating efficacy.
Drug: progesterone
Target: Cation channel sperm-associated protein 3 (Ion channel)
Gene: CATSPER3
UniProt: Q86XQ3 (CTSR3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.11
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluorometry, 2-3&micro;M shows the saturating efficacy.
Drug: progesterone
Target: Cation channel sperm-associated protein 4 (Ion channel)
Gene: CATSPER4
UniProt: Q7RTX7 (CTSR4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.11
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology, kinetic rapid mixing fluorometry, 2-3&micro;M shows the saturating efficacy.
Drug: progesterone
Target: Short transient receptor potential channel 5 (Ion channel)
Gene: TRPC5
UniProt: Q9UL62 (TRPC5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Action type: BLOCKER
Drug: progesterone
Target: P2X purinoceptor 3 (Ion channel)
Gene: P2RX3
UniProt: P56373 (P2RX3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.8
Assay: Antagonist activity at human P2X3 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced calcium flux measured for 30 secs at 0.4 secs intervals by Flou-4-AM dye based fluorescence assay
Drug: proglumide
Target: Histamine H2 receptor (GPCR)
Gene: Hrh2
UniProt: P25102 (HRH2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 2.6
Assay: Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro
Drug: proglumide
Target: Gastrin/cholecystokinin type B receptor (GPCR)
Gene: CCKBR
UniProt: P32239 (GASR_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action
Drug: proguanil
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: Q0IJY2 (Q0IJY2_PLAMA)
Organism: Plasmodium malariae
Drug: proguanil
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: O02604 (DRTS_PLAVI)
Organism: Plasmodium vivax
Drug: proguanil
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: P13922 (DRTS_PLAFK)
Organism: Plasmodium falciparum
Action type: INHIBITOR
Drug: proguanil
Target: Trace amine-associated receptor 1 (GPCR)
Gene: Taar1
UniProt: Q923Y8 (TAAR1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 5.27
Assay: Agonist activity at mouse TAAR1 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay
Drug: promazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.909
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: promazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.704
Action type: ANTAGONIST
Drug: promazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: promazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.943
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: promazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.337
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: promazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.886
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: promazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.529
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: promazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.796
Action type: ANTAGONIST
Drug: promazine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.656
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: promazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.284
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: promazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.896
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: promazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.226
Drug: promazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Drug: promazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.799
Action type: ANTAGONIST
Drug: promazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Drug: promazine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.551
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: promazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.825
Drug: promazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.412
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.056
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.377
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.337
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promazine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.796
Drug: promazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.432
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: promazine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: promazine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.427
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: promazine
Target: Major prion protein (Surface antigen)
Gene: PRNP
UniProt: P04156 (PRIO_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.3
Assay: Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
Drug: promazine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.76
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: promazine
Target: Trypanothione reductase (Enzyme)
Gene: TPR
UniProt: P28593 (TYTR_TRYCR)
Organism: Trypanosoma cruzi
Activity: Ki = 4.23
Assay: Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type)
Drug: promazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.344
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: promazine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.806
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: promazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.03
Drug: promazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.29
Drug: promazine
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.9
Assay: Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting
Drug: promazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 4.95
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: promazine
Target: Dopamine receptor (GPCR)
Gene: DRD2|DRD1
UniProt: P20288|Q95136 (DRD2_BOVIN|DRD1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.89
Assay: Compound was tested for inhibition of [3H]spiperone binding in membrane preparations obtained from calf caudate.
Drug: promazine
Target: Dopamine receptor (GPCR)
Gene: Drd1|Drd3|Drd5|Drd4|Drd2
UniProt: P18901|P19020|P25115|P30729|P61169 (DRD1_RAT|DRD3_RAT|DRD5_RAT|DRD4_RAT|DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.98
Assay: Compound was tested for inhibition of [3H]spiperone binding in membrane preparations obtained from rat corpus striatum.
Drug: promazine
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 = 5.27
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: promazine
Target: FAD-linked sulfhydryl oxidase ALR (Enzyme)
Gene: GFER
UniProt: P55789 (ALR_HUMAN)
Organism: Homo sapiens
Activity: AC50 = 5.89
Assay: PUBCHEM_BIOASSAY: HTS-Luminescent assay for inhibitors of ALR by detection of hydrogen peroxide production Measured in Biochemical System Using Plate Reader - 2036-02_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488787]
Drug: promegestone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.4
Assay: Binding affinity to progesterone receptor
Drug: promegestone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.88
Assay: Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
Drug: promethazine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.863
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: promethazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.609
Drug: promethazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.592
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: promethazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.921
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: promethazine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.12
Assay: Binding affinity to SERT (unknown origin) by radioligand binding assay
Drug: promethazine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.376
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: promethazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.829
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: promethazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Drug: promethazine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.367
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: promethazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.188
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: promethazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.948
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: promethazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Drug: promethazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.62
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: promethazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.721
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: promethazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.62
Action type: ANTAGONIST
Drug: promethazine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.941
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: promethazine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.823
Drug: promethazine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.479
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promethazine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.921
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promethazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.382
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promethazine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.975
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promethazine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.48
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: promethazine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.292
Drug: promethazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.452
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: promethazine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.42
Drug: promethazine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.495
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: promethazine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P06276 (CHLE_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.1
Drug: promethazine
Target: Major prion protein (Surface antigen)
Gene: PRNP
UniProt: P04156 (PRIO_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.1
Assay: Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells
Drug: promethazine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.45
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: promethazine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.678
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: promethazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.1
Drug: promethazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.59
Drug: promethazine
Target: Pleiotropic ABC efflux transporter of multiple drugs (Transporter)
Gene: PDR5
UniProt: P33302 (PDR5_YEAST)
Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c)
Activity: IC50 = 4.75
Assay: Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
Drug: promethazine
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 = 5.16
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