tamoxifen [Ligand Id: 1016] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL83 (ICI-46474, ICI-47699, Mammaton, Nolvadex, Novaldex, NSC-727681, Soltamox, Tamoplex, Tamoxifen, Tamoxifene, Tamoxifeno)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • aldehyde oxidase 1/Aldehyde oxidase in Human [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
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  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • glucosylceramidase beta/Beta-glucocerebrosidase in Human [ChEMBL: CHEMBL2179] [GtoPdb: 2978] [UniProtKB: P04062]
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  • B2 receptor/Bradykinin B2 receptor in Human [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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  • Estrogen-related receptor-α/Estrogen-related receptor alpha in Human [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • Serine/threonine protein phosphatase 2B catalytic subunit, alpha isoform in Human [ChEMBL: CHEMBL4445] [UniProtKB: Q08209]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Transcriptional activator protein luxR in Aliivibrio fischeri [ChEMBL: CHEMBL5351] [UniProtKB: P12746]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • GPER in Human [GtoPdb: 221] [UniProtKB: Q99527]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
ChEMBL Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand B 8.3 pKi 5 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 4.86 pKi 13864 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 4.62 pIC50 23767 nM IC50 DrugMatrix in vitro pharmacology data
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 5.4 pKi 3985 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 5.15 pIC50 7099 nM IC50 DrugMatrix in vitro pharmacology data
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.68 pKi 2092 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.43 pIC50 3701 nM IC50 DrugMatrix in vitro pharmacology data
aldehyde oxidase 1/Aldehyde oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3257] [GtoPdb: 3186] [UniProtKB: Q06278]
ChEMBL Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis B 4.01 pIC50 97300 nM IC50 WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (2018)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.05 pKi 8925 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 4.66 pIC50 22050 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.61 pKi 2449 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.3 pIC50 4982 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.14 pKi 726 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.71 pIC50 1935 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.79 pKi 1606 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.45 pIC50 3518 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.82 pKi 15108 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.64 pIC50 22662 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 4.92 pIC50 12022.64 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
Anti-estrogen binding site (AEBS) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL612409] [UniProtKB: Q15125, Q9UBM7]
ChEMBL Binding affinity towards antiestrogen binding site AEBS B 9 pKd 1 nM Kd J Med Chem (2003) 46: 883-908 [PMID:12620065]
ChEMBL Displacement of [3H]tamoxifen from antiestrogen binding site (AEBS) B 7.92 pIC50 12 nM IC50 J Med Chem (1989) 32: 192-197 [PMID:2909731]
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 5 pKi 9984 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 4.76 pIC50 17289 nM IC50 DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 5.24 pKi 5778 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 5.11 pIC50 7703 nM IC50 DrugMatrix in vitro pharmacology data
glucosylceramidase beta/Beta-glucocerebrosidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2179] [GtoPdb: 2978] [UniProtKB: P04062]
ChEMBL Chaperone activity at GCase in wild-type human fibroblasts assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay B 5.6 pEC50 2500 nM EC50 Bioorg Med Chem Lett (2020) 30: 126806-126806 [PMID:31757667]
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) F 4.63 pIC50 23300 nM IC50 Pharm Res (2003) 20: 537-544 [PMID:12739759]
ChEMBL TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP) F 4.81 pIC50 15400 nM IC50 Pharm Res (2003) 20: 537-544 [PMID:12739759]
B2 receptor/Bradykinin B2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411]
ChEMBL DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin) B 4.92 pKi 12048 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin) B 4.69 pIC50 20356 nM IC50 DrugMatrix in vitro pharmacology data
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
ChEMBL Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 5.82 pKi 1500 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.36 pIC50 4391 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.33 pKi 4702 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 4.87 pIC50 13339 nM IC50 DrugMatrix in vitro pharmacology data
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.37 pKi 4251 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.07 pIC50 8502 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.33 pKi 4628 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 4.86 pIC50 13885 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.44 pKi 364 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.97 pIC50 1072 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 5.41 pKi 3913 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone) B 4.95 pIC50 11161 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.84 pKi 1462 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.73 pIC50 1841 nM IC50 DrugMatrix in vitro pharmacology data
Emopamil-binding protein-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2311238] [UniProtKB: Q9BY08]
ChEMBL Binding affinity to emopamil binding protein (unknown origin) B 8.55 pKi 2.8 nM Ki Bioorg Med Chem (2013) 21: 215-222 [PMID:23199475]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.45 pIC50 3553 nM IC50 DrugMatrix in vitro pharmacology data
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting B 7.51 pKi 31.19 nM Ki Bioorg Med Chem (2010) 18: 5593-5601 [PMID:20621492]
GtoPdb - - 7.8 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
GtoPdb - - 7.82 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
ChEMBL Antagonist activity at ERalpha receptor in human MCF7 cells B 5 pIC50 10000 nM IC50 J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
ChEMBL Displacement of fluorescent estrogen ligand from recombinant human ERalpha expressed in insect cells incubated for 2 hrs by polarization B 5.57 pIC50 2670 nM IC50 Eur J Med Chem (2017) 140: 252-273 [PMID:28942113]
ChEMBL Antagonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay F 5.6 pIC50 2540 nM IC50 Eur J Med Chem (2012) 54: 188-196 [PMID:22647217]
ChEMBL Antagonist activity at ERalpha expressed in yeast assessed as inhibition of E2-induced alpha-galactosidase activity F 5.6 pIC50 2540 nM IC50 J Med Chem (2010) 53: 5361-5365 [PMID:20553023]
ChEMBL Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay B 5.79 pIC50 1605 nM IC50 J Med Chem (2017) 60: 2790-2818 [PMID:28296398]
ChEMBL Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay B 5.79 pIC50 1605 nM IC50 J Med Chem (2018) 61: 2837-2864 [PMID:29562737]
ChEMBL Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells measured after 2 hrs by fluorescence polarization assay B 5.81 pIC50 1560 nM IC50 Eur J Med Chem (2019) 161: 445-455 [PMID:30384047]
ChEMBL Displacement of Fluormone ES2 Green from full length human ER-alpha expressed in insect cells after 2 hrs by fluorescence polarization assay B 5.85 pIC50 1420 nM IC50 Eur J Med Chem (2018) 150: 783-795 [PMID:29587221]
ChEMBL Displacement of fluorescein-labeled estrogen ligand from recombinant ER-alpha (unknown origin) incubated for 2 hrs by fluorescence polarization assay B 6 pIC50 1000 nM IC50 Eur J Med Chem (2016) 118: 328-339 [PMID:27176944]
ChEMBL Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay B 6.21 pIC50 622 nM IC50 J Med Chem (2005) 48: 364-379 [PMID:15658851]
ChEMBL Inhibitory concentration against estrogen receptor alpha using estrogen response element (ERE) assay. B 6.21 pIC50 622 nM IC50 J Med Chem (2003) 46: 2945-2957 [PMID:12825935]
ChEMBL Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50% F 6.3 pIC50 500 nM IC50 J Med Chem (2002) 45: 5358-5364 [PMID:12431063]
ChEMBL Antagonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay B 6.47 pIC50 341 nM IC50 Bioorg Med Chem (2017) 25: 5216-5237 [PMID:28882502]
ChEMBL Displacement of [3H]E2 from GST-fused ERalpha-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method B 6.65 pIC50 226 nM IC50 Bioorg Med Chem (2017) 25: 5216-5237 [PMID:28882502]
ChEMBL Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay B 6.65 pIC50 222 nM IC50 Bioorg Med Chem (2016) 24: 5495-5504 [PMID:27647375]
ChEMBL Inhibition of estrogen receptor (unknown origin) B 6.65 pIC50 222 nM IC50 Eur J Med Chem (2018) 143: 515-531 [PMID:29207335]
ChEMBL Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2009) 19: 1218-1223 [PMID:19131248]
ChEMBL Displacement of [3H]E2 from human recombinant ERalpha assessed as receptor binding after 45 mins by scintillation counting method B 7 pIC50 100 nM IC50 Eur J Med Chem (2018) 143: 515-531 [PMID:29207335]
ChEMBL Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in baculovirus infected insect cells incubated in dark for 2 hrs by Beacon single-tube fluorescent polarization assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2020) 28: 115261-115261 [PMID:31987694]
ChEMBL Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2008) 16: 9554-9573 [PMID:18835176]
ChEMBL Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor alpha after 2 hrs by fluorescence polarization assay B 7.15 pIC50 70 nM IC50 J Med Chem (2018) 61: 514-534 [PMID:28426931]
ChEMBL Displacement of fluorescent labeled-ligand from ERalpha (unknown origin) by competitive binding assay B 7.16 pIC50 69 nM IC50 Bioorg Med Chem Lett (2021) 52: 128383-128383 [PMID:34592434]
ChEMBL Displacement of fluorescein-labeled estrogen from human recombinant ERalpha by fluorescence polarization based competitive binding affinity assay B 7.21 pIC50 61 nM IC50 J Med Chem (2014) 57: 9370-9382 [PMID:25369367]
ChEMBL Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor alpha expressed in Spodoptera frugiperda by fluorescence polarization assay B 7.22 pIC50 60.9 nM IC50 J Med Chem (2018) 61: 514-534 [PMID:28426931]
ChEMBL Binding affinity to human ERalpha B 7.22 pIC50 60.9 nM IC50 J Med Chem (2014) 57: 9370-9382 [PMID:25369367]
ChEMBL Antagonist activity at ERalpha (unknown origin) B 7.22 pIC50 60.9 nM IC50 Bioorg Med Chem (2020) 28: 115261-115261 [PMID:31987694]
ChEMBL Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assay B 7.24 pIC50 58 nM IC50 J Med Chem (2021) 64: 11841-11856 [PMID:34251202]
ChEMBL Displacement of [3H]17-beta-estradiol from human estrogen receptor alpha B 7.38 pIC50 42 nM IC50 J Med Chem (1999) 42: 3126-3133 [PMID:10447957]
ChEMBL Antagonist activity at Gal4 DBD-fused human ERalpha LBD expressed in HEK293T cells assessed as inhibition of estradiol-induced transcriptional activation after 20 hrs by luciferase reporter gene assay B 7.41 pIC50 39 nM IC50 J Med Chem (2013) 56: 5782-5796 [PMID:23786452]
ChEMBL Binding affinity to ERalpha receptor (unknown origin) B 7.61 pIC50 24.55 nM IC50 J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
ChEMBL Displacement of radioligand from Estrogen receptor alpha B 8.08 pIC50 8.4 nM IC50 Bioorg Med Chem Lett (2002) 12: 1283-1285 [PMID:11965371]
ChEMBL Displacement of [3H]-E2 from human ER-alpha incubated for 16 to 20 hrs by liquid scintillation counting analysis B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2016) 112: 171-179 [PMID:26896706]
ChEMBL Inhibition of estrogen receptor-alpha (unknown origin) by ELISA B 8.82 pIC50 1.5 nM IC50 Eur J Med Chem (2019) 166: 281-290 [PMID:30731397]
ChEMBL Antagonist activity at human estrogen receptor-alpha by yeast two-hybrid assay in presence of SRC1 B 5.6 pEC50 2540 nM EC50 Bioorg Med Chem Lett (2013) 23: 3329-3333 [PMID:23608764]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
GtoPdb - - 7.16 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
GtoPdb - - 7.17 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
ChEMBL Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation counting B 9.29 pKi 0.51 nM Ki ACS Med Chem Lett (2012) 3: 207-210 [PMID:22582136]
ChEMBL Antagonist activity at ERbeta expressed in yeast assessed as inhibition of E2-induced alpha-galactosidase activity F 5.78 pIC50 1660 nM IC50 J Med Chem (2010) 53: 5361-5365 [PMID:20553023]
ChEMBL Antagonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay F 5.78 pIC50 1660 nM IC50 Eur J Med Chem (2012) 54: 188-196 [PMID:22647217]
ChEMBL Antagonist activity at full length ERbeta (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay B 5.82 pIC50 1530 nM IC50 Bioorg Med Chem (2017) 25: 5216-5237 [PMID:28882502]
ChEMBL Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay B 6 pIC50 >1000 nM IC50 J Med Chem (2005) 48: 364-379 [PMID:15658851]
ChEMBL Inhibitory concentration against estrogen receptor 2 using estrogen response element (ERE) assay. B 6 pIC50 >1000 nM IC50 J Med Chem (2003) 46: 2945-2957 [PMID:12825935]
ChEMBL Displacement of fluorescein-labeled estrogen from human recombinant ERbeta by fluorescence polarization based competitive binding affinity assay B 6.72 pIC50 190 nM IC50 J Med Chem (2014) 57: 9370-9382 [PMID:25369367]
ChEMBL Antagonist activity at ERbeta (unknown origin) B 6.73 pIC50 188 nM IC50 Bioorg Med Chem (2020) 28: 115261-115261 [PMID:31987694]
ChEMBL Binding affinity to human ERbeta B 6.73 pIC50 188 nM IC50 J Med Chem (2014) 57: 9370-9382 [PMID:25369367]
ChEMBL Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor beta expressed in insect cells by fluorescence polarization assay B 6.73 pIC50 188 nM IC50 J Med Chem (2018) 61: 514-534 [PMID:28426931]
ChEMBL Displacement of [3H]-E2 from human ER-beta incubated for 16 to 20 hrs by liquid scintillation counting analysis B 6.74 pIC50 180 nM IC50 Eur J Med Chem (2016) 112: 171-179 [PMID:26896706]
ChEMBL Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence polarization assay B 6.77 pIC50 170 nM IC50 J Med Chem (2018) 61: 514-534 [PMID:28426931]
ChEMBL Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay B 6.77 pIC50 170 nM IC50 Bioorg Med Chem (2008) 16: 9554-9573 [PMID:18835176]
ChEMBL Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERbeta expressed in baculovirus infected insect cells incubated in dark for 2 hrs by Beacon single-tube fluorescent polarization assay B 6.77 pIC50 170 nM IC50 Bioorg Med Chem (2020) 28: 115261-115261 [PMID:31987694]
ChEMBL Displacement of [3H]E2 from GST-fused ERbeta-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method B 7.1 pIC50 79.7 nM IC50 Bioorg Med Chem (2017) 25: 5216-5237 [PMID:28882502]
ChEMBL Antagonist activity at human estrogen receptor-beta by yeast two-hybrid assay in presence of SRC1 B 5.78 pEC50 1660 nM EC50 Bioorg Med Chem Lett (2013) 23: 3329-3333 [PMID:23608764]
Estrogen-related receptor-α/Estrogen-related receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474]
ChEMBL Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method B 6.7 pIC50 200 nM IC50 J Med Chem (2013) 56: 2779-2790 [PMID:23448346]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 6.1 pKi 792.2 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human ERG B 5.8 pIC50 1584.89 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 6.01 pIC50 967 nM IC50 DrugMatrix in vitro pharmacology data
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.03 pKi 9240 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.03 pIC50 9396 nM IC50 DrugMatrix in vitro pharmacology data
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.2 pKi 6252 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.81 pIC50 15629 nM IC50 DrugMatrix in vitro pharmacology data
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
ChEMBL DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.76 pKi 17329 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.7 pIC50 19856 nM IC50 DrugMatrix in vitro pharmacology data
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.53 pKi 29308 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.52 pIC50 30481 nM IC50 DrugMatrix in vitro pharmacology data
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.6 pKi 24886 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH) B 4.58 pIC50 26529 nM IC50 DrugMatrix in vitro pharmacology data
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.15 pKi 7142 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 4.75 pIC50 17594 nM IC50 DrugMatrix in vitro pharmacology data
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.17 pKi 681 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.55 pIC50 2829 nM IC50 DrugMatrix in vitro pharmacology data
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.56 pKi 2771 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.11 pIC50 7793 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.2 pKi 630 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.53 pIC50 2974 nM IC50 DrugMatrix in vitro pharmacology data
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.17 pKi 672 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.32 pIC50 4817 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.73 pKi 1857 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.59 pIC50 2585 nM IC50 DrugMatrix in vitro pharmacology data
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P) B 5.07 pKi 8540 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P) B 4.81 pIC50 15656 nM IC50 DrugMatrix in vitro pharmacology data
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.91 pKi 1223 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.44 pIC50 3670 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.84 pKi 1459 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.83 pIC50 1472 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 7 pKi 100 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 4.5 pIC50 31400 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: transepithelial transport of Rhodamine 123 (basal to apical) in Caco-2 cells F 4.54 pIC50 29000 nM IC50 Biopharm Drug Dispos (2004) 25: 283-289 [PMID:15386482]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 4.92 pIC50 12100 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.19 pIC50 6400 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells B 4.25 pEC50 56500 nM EC50 Bioorg Med Chem Lett (2008) 18: 3741-3744 [PMID:18524592]
PLD1/Phospholipase D1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308939] [GtoPdb: 1433] [UniProtKB: P70496]
ChEMBL Inhibition of N-terminally truncated rat PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay B 4.7 pIC50 >20000 nM IC50 Nat Chem Biol (2009) 5: 108-117 [PMID:19136975]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Agonist activity at progesterone receptor in human MCF7 cells B 4 pIC50 >100000 nM IC50 J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
ChEMBL Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response B 6.89 pIC50 128.82 nM IC50 J Med Chem (2015) 58: 8128-8140 [PMID:26407012]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.59 pKi 2589 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 4.7 pIC50 19846 nM IC50 DrugMatrix in vitro pharmacology data
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.53 pIC50 2949 nM IC50 DrugMatrix in vitro pharmacology data
Serine/threonine protein phosphatase 2B catalytic subunit, alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4445] [UniProtKB: Q08209]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP) B 4.51 pIC50 30573 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.16 pKi 6949 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 4.92 pIC50 12160 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.86 pKi 1372 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.32 pIC50 4801 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.88 pKi 1326 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.68 pIC50 2084 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.62 pKi 241 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.34 pIC50 460 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.91 pKi 1244 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting B 5.98 pKi 1041 nM Ki J Med Chem (2012) 55: 5704-5719 [PMID:22537153]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.57 pIC50 2679 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.91 pKi 1240 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.63 pIC50 2334 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 7.46 pKi 35 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 8.06 pKi 8.71 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 7.68 pIC50 21 nM IC50 DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 6.04 pIC50 916 nM IC50 DrugMatrix in vitro pharmacology data
Transcriptional activator protein luxR in Aliivibrio fischeri (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5351] [UniProtKB: P12746]
ChEMBL Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity B 4.4 pIC50 40000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4355-4358 [PMID:20615699]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.92 pIC50 1195 nM IC50 DrugMatrix in vitro pharmacology data
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.1 pIC50 8033 nM IC50 DrugMatrix in vitro pharmacology data
GPER in Human [GtoPdb: 221] [UniProtKB: Q99527]
GtoPdb - - 6 pKi - - - Endocrinology (2005) 146: 624-32 [PMID:15539556]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]