raloxifene [Ligand Id: 2820] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL81 (Eviden, Evista, J22.982B, Keoxifene, LY-139481, NSC-747974, Raloxifene, Raloxifeno, Raloxiphene, Raxeto)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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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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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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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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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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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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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
  • Estrogen receptor-α/Estrogen receptor alpha in Rat [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
  • Estrogen receptor-β/Estrogen receptor beta in Rat [ChEMBL: CHEMBL3021] [GtoPdb: 621] [UniProtKB: Q62986]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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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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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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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 9 pKi 1 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) B 6.4 pIC50 400 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 5.93 pKi 1185 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) B 5.68 pIC50 2111 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 Uncompetitive type inhibition of human AOX assessed as inhibitor dissociation constant by measuring intercept of the double reciprocal plot using phenanthridine as substrate by spectrophotometry based Lineweaver-Burk plot analysis B 8.15 pKi 0.01 uM Kii J Med Chem (2021) 64: 13025-13037 [PMID:34415167]
ChEMBL Uncompetitive type inhibition of human AOX assessed as inhibition constant using phthalazine as substrate preincubated for 30 mins followed by substrate addition by HPLC-MS analysis B 9.06 pKi 0.87 nM Ki J Med Chem (2021) 64: 13025-13037 [PMID:34415167]
ChEMBL Uncompetitive type inhibition of human AOX assessed as inhibition constant using vanillin as substrate by HPLC-MS analysis B 9.06 pKi 0.87 nM Ki J Med Chem (2021) 64: 13025-13037 [PMID:34415167]
ChEMBL Uncompetitive type inhibition of human AOX assessed as inhibition constant using nicotine-1(S)-iminium ion as substrate incubated for 2 mins by HPLC-MS analysis B 9.06 pKi 0.87 nM Ki J Med Chem (2021) 64: 13025-13037 [PMID:34415167]
GtoPdb - - 7.35 pIC50 44.5 nM IC50 WO2018198842A1. Therapeutic agent for nonalcoholic fatty liver disease (2018)
ChEMBL Inhibition of aldehyde oxidase in human liver cytosolic fraction using methyl-nicotinamide substrate incubated for 120 mins by HPLC analysis B 7.35 pIC50 44.5 nM IC50 WO-2018198842-A1. Therapeutic agent for nonalcoholic fatty liver disease (2018)
ChEMBL Inhibition of human AOX using phthalazine as substrate preincubated for 30 mins followed by substrate addition by HPLC-MS analysis B 8.24 pIC50 5.7 nM IC50 Eur J Med Chem (2020) 187: 111948-111948 [PMID:31877540]
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 6.05 pKi 892 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.66 pIC50 2204 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.83 pKi 1491 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.57 pIC50 2693 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 6.32 pKi 478 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.01 pIC50 973 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 6.2 pKi 624 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.78 pIC50 1664 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 5.77 pKi 1688 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.43 pIC50 3698 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.97 pKi 107 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.13 pIC50 738 nM IC50 DrugMatrix in vitro pharmacology data
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay B 4.94 pIC50 11560 nM IC50 Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
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 7.18 pKi 66 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes assessed as inhibition constant incubated for 1 hr by TopCount liquid scintillation counting analysis B 6.62 pKi ~240 nM Ki J Nat Prod (2023) 86: 1786-1792 [PMID:37450763]
Complement C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364163] [UniProtKB: P01031]
ChEMBL Binding affinity to human C5a assessed as dissociation constant after 1 hr by circular dichroism analysis B 6.15 pKd 710 nM Kd Bioorg Med Chem (2019) 27: 115052-115052 [PMID:31447248]
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
ChEMBL Inhibition of Trypanosoma cruzi cruzain by quantitative high throughput screening B 4.22 pIC50 >60000 nM IC50 J Med Chem (2010) 53: 37-51 [PMID:19908840]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 B 4.48 pIC50 33000 nM IC50 J Med Chem (2010) 53: 4259-4265 [PMID:20426472]
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.7 pIC50 2000 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 5.63 pKi 2342 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 5.18 pIC50 6644 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 5.71 pKi 1932 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.41 pIC50 3864 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 6.41 pKi 391 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.93 pIC50 1174 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 6.27 pKi 531 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.81 pIC50 1565 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 5.83 pKi 1485 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.73 pIC50 1869 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 [3H]estradiol from full length biotinylated human ERalpha by scintillation proximity assay B 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2008) 18: 5075-5077 [PMID:18722117]
ChEMBL Binding affinity to ERalpha (unknown origin) B 9.37 pKi 0.43 nM Ki Bioorg Med Chem (2016) 24: 759-767 [PMID:26795112]
ChEMBL Binding affinity for estrogen receptor alpha B 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (2003) 13: 1907-1910 [PMID:12749895]
ChEMBL Binding affinity to ERalpha ligand binding domain B 9.42 pKi 0.38 nM Ki ACS Med Chem Lett (2012) 3: 207-210 [PMID:22582136]
ChEMBL Displacement of [3H]estradiol from ERalpha after 4 hrs by scintillation counting B 9.43 pKi 0.37 nM Ki ACS Med Chem Lett (2012) 3: 207-210 [PMID:22582136]
GtoPdb - - 9.5 pKi - - - Endocrinology (1997) 138: 863-70 [PMID:9048584]
GtoPdb - - 9.5 pKi - - - J Med Chem (2000) 43: 4934-47 [PMID:11150164]
ChEMBL Ability to displace [3H]17-beta-estradiol from Estrogen receptor alpha by scintillation proximity assay. B 9.66 pKi 0.22 nM Ki Bioorg Med Chem Lett (2001) 11: 1939-1942 [PMID:11459665]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.8 pKi 0.16 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Antagonistic activity against estrogen receptor alpha in presence of 0.1 nM estradiol F 10.52 pKi 0.03 nM Ki J Med Chem (2005) 48: 5989-6003 [PMID:16162002]
ChEMBL Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine incorporation assay F 6.65 pIC50 222 nM IC50 J Med Chem (2009) 52: 7544-7569 [PMID:19366247]
ChEMBL Antagonist activity at ERalpha in human MCF7 cells assessed as downregulation of ERalpha B 7 pIC50 >100 nM IC50 Eur J Med Chem (2022) 227: 113869-113869 [PMID:34710747]
ChEMBL Antagonist activity at human ERalpha E353A mutant expressed in HEK293T cells co-expressing ERE assessed as inhibition of ES8-induced transactivation by luciferase reporter gene assay F 7.25 pIC50 56 nM IC50 Bioorg Med Chem Lett (2010) 20: 5258-5261 [PMID:20659801]
ChEMBL Binding affinity to human recombinant ERalpha by competitive fluorometric binding assay B 7.27 pIC50 54 nM IC50 Bioorg Med Chem Lett (2022) 64: 128668-128668 [PMID:35276362]
ChEMBL Antagonist activity at estrogen receptor in human Ishikawa cells assessed as 17-beta-estradiol-induced alkaline phosphatase activity after 3 days by chemiluminescence assay F 7.62 pIC50 24 nM IC50 J Med Chem (2009) 52: 7544-7569 [PMID:19366247]
ChEMBL Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells B 7.66 pIC50 22 nM IC50 J Med Chem (2005) 48: 364-379 [PMID:15658851]
ChEMBL Displacement of [3H]estradiol from human recombinant ERalpha B 7.69 pIC50 20.6 nM IC50 J Med Chem (2007) 50: 2682-2692 [PMID:17489582]
ChEMBL In vitro binding affinity for estrogen receptor alpha B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2003) 13: 1919-1922 [PMID:12749898]
ChEMBL Antagonist activity at ER-alpha in human MCF-7:WS8 cells transfected with an estrogen response element assessed as suppression of estrogen-induced response incubated for 18 hrs by luciferase reporter gene assay B 8.23 pIC50 5.9 nM IC50 J Med Chem (2020) 63: 11085-11099 [PMID:32886512]
ChEMBL In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha B 8.4 pIC50 4 nM IC50 J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay B 8.62 pIC50 2.4 nM IC50 J Med Chem (2005) 48: 364-379 [PMID:15658851]
ChEMBL Inhibition of binding to recombinant human ERalpha by scintillation proximity assay B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2005) 15: 5124-5128 [PMID:16203138]
ChEMBL Binding affinity towards human recombinant Estrogen receptor alpha was determined B 8.74 pIC50 1.8 nM IC50 J Med Chem (2004) 47: 2171-2175 [PMID:15084115]
ChEMBL Displacement of [3H]17-beta-estradiol from full length human estrogen receptor alpha B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2004) 14: 2741-2745 [PMID:15125925]
ChEMBL Binding affinity for Human Estrogen receptor-alpha B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2003) 13: 479-483 [PMID:12565955]
ChEMBL Binding affinity against human estrogen receptor alpha in competitive binding assay B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2004) 14: 1417-1421 [PMID:15006374]
ChEMBL Inhibition of bindign to recombinant human estrogen receptor alpha B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2005) 15: 107-113 [PMID:15582421]
ChEMBL Binding potency for human ER alpha B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2004) 14: 3861-3864 [PMID:15225685]
ChEMBL Binding potency for human ER alpha B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2004) 14: 3865-3868 [PMID:15225686]
ChEMBL Binding affinity towards human estrogen receptor alpha B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem Lett (2004) 14: 2551-2554 [PMID:15109649]
ChEMBL Binding affinity to ERalpha B 8.74 pIC50 1.8 nM IC50 J Med Chem (2006) 49: 3056-3059 [PMID:16722623]
ChEMBL Displacement of radiolabeled estrogen from estrogen receptor alpha by scintillation counting B 8.74 pIC50 1.8 nM IC50 J Med Chem (2009) 52: 7544-7569 [PMID:19366247]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha B 9.05 pIC50 0.89 nM IC50 Bioorg Med Chem Lett (2005) 15: 2891-2893 [PMID:15911274]
ChEMBL Antagonist activity at ERalpha (unknown origin) B 9.13 pIC50 0.74 nM IC50 Eur J Med Chem (2022) 227: 113869-113869 [PMID:34710747]
ChEMBL Inhibition of estrogen receptor alpha B 9.14 pIC50 0.73 nM IC50 Bioorg Med Chem Lett (2005) 15: 1505-1507 [PMID:15713417]
ChEMBL In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol F 9.14 pIC50 0.72 nM IC50 J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL In vitro inhibition of transcriptional activation induced by 1 nM 17-beta estradiol in T47D cells expressing estrogen receptor alpha B 9.15 pIC50 0.7 nM IC50 J Med Chem (2002) 45: 5492-5505 [PMID:12459017]
ChEMBL DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) B 9.26 pIC50 0.55 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of Fluormone ES2 from human recombinant full length untagged-ERalpha by fluorescence polarization competition binding assay B 9.33 pIC50 0.47 nM IC50 Bioorg Med Chem (2016) 24: 2914-2919 [PMID:27185013]
ChEMBL Antagonist activity at human ERalpha expressed in african green monkey CV1 cells assessed as inhibition of estrogen like activity after 24 hrs by luciferase reporter gene assay F 9.34 pIC50 0.46 nM IC50 J Nat Prod (2006) 69: 247-250 [PMID:16499324]
ChEMBL Antagonist activity at human wild type ERalpha expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay F 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (2010) 20: 5258-5261 [PMID:20659801]
ChEMBL Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay B 9.74 pIC50 0.18 nM IC50 Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor alpha. B 7.66 pEC50 22 nM EC50 J Med Chem (2002) 45: 1399-1401 [PMID:11906280]
ChEMBL Activity against estrogen receptor alpha B 7.66 pEC50 22 nM EC50 J Med Chem (2008) 51: 3661-3680 [PMID:18457385]
ChEMBL Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay B 9.18 pEC50 0.66 nM EC50 Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565]
Estrogen receptor-α/Estrogen receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2724] [GtoPdb: 620] [UniProtKB: P06211]
ChEMBL Binding to Estrogen receptor- alpha (ER alpha) receptor B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2002) 12: 2875-2878 [PMID:12270167]
ChEMBL Binding affinity for Rat Estrogen receptor-alpha B 9.15 pIC50 0.7 nM IC50 Bioorg Med Chem Lett (2003) 13: 479-483 [PMID:12565955]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Displacement of [3H]estradiol from full length biotinylated human ERbeta by scintillation proximity assay B 7.64 pKi 23 nM Ki Bioorg Med Chem Lett (2008) 18: 5075-5077 [PMID:18722117]
GtoPdb - - 8 pKi 10 nM Ki Bioorg Med Chem Lett (2001) 11: 1939-42 [PMID:11459665]
ChEMBL Ability to displace [3H]17-beta-estradiol from Estrogen receptor beta by scintillation proximity assay. B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2001) 11: 1939-1942 [PMID:11459665]
ChEMBL Antagonistic activity against estrogen receptor beta in presence of 0.1 nM estradiol F 8.35 pKi 4.5 nM Ki J Med Chem (2005) 48: 5989-6003 [PMID:16162002]
ChEMBL Binding affinity for estrogen receptor beta B 8.37 pKi 4.3 nM Ki Bioorg Med Chem Lett (2003) 13: 1907-1910 [PMID:12749895]
ChEMBL Binding affinity to ERbeta (unknown origin) B 8.37 pKi 4.3 nM Ki Bioorg Med Chem (2016) 24: 759-767 [PMID:26795112]
ChEMBL Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation counting B 8.56 pKi 2.74 nM Ki ACS Med Chem Lett (2012) 3: 207-210 [PMID:22582136]
ChEMBL Antagonist activity at ERbeta (unknown origin) B 5.13 pIC50 7430 nM IC50 Eur J Med Chem (2022) 227: 113869-113869 [PMID:34710747]
ChEMBL Binding affinity to human recombinant ERbeta by competitive fluorometric binding assay B 5.85 pIC50 1420 nM IC50 Bioorg Med Chem Lett (2022) 64: 128668-128668 [PMID:35276362]
ChEMBL Antagonist activity at human ERbeta E305A mutant expressed in HEK293T cells co-expressing ERE assessed as inhibition of ES8-induced transactivation by luciferase reporter gene assay F 6.24 pIC50 577 nM IC50 Bioorg Med Chem Lett (2010) 20: 5258-5261 [PMID:20659801]
ChEMBL Displacement of [3H]estradiol from human recombinant ERbeta B 6.25 pIC50 557 nM IC50 J Med Chem (2007) 50: 2682-2692 [PMID:17489582]
ChEMBL In vitro binding affinity for estrogen receptor beta B 6.33 pIC50 470 nM IC50 Bioorg Med Chem Lett (2003) 13: 1919-1922 [PMID:12749898]
ChEMBL Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay B 6.47 pIC50 341 nM IC50 J Med Chem (2005) 48: 364-379 [PMID:15658851]
ChEMBL Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells B 6.59 pIC50 260 nM IC50 J Med Chem (2005) 48: 364-379 [PMID:15658851]
ChEMBL In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 B 7.37 pIC50 43 nM IC50 J Med Chem (2001) 44: 1654-1657 [PMID:11356100]
ChEMBL Inhibition of estrogen receptor beta B 7.72 pIC50 18.9 nM IC50 Bioorg Med Chem Lett (2005) 15: 1505-1507 [PMID:15713417]
ChEMBL In vitro inhibition of 1 nM 17-beta-estradiol induced transcriptional activation in T47D cells expressing estrogen receptor beta B 7.82 pIC50 15 nM IC50 J Med Chem (2002) 45: 5492-5505 [PMID:12459017]
ChEMBL Binding potency for human ER beta B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2004) 14: 3865-3868 [PMID:15225686]
ChEMBL Binding affinity towards human recombinant Estrogen receptor beta was determined B 7.92 pIC50 12 nM IC50 J Med Chem (2004) 47: 2171-2175 [PMID:15084115]
ChEMBL Displacement of [3H]17-beta-estradiol from full length human estrogen receptor beta B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2004) 14: 2741-2745 [PMID:15125925]
ChEMBL Binding affinity for Human Estrogen receptor-beta B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2003) 13: 479-483 [PMID:12565955]
ChEMBL Binding affinity against human estrogen receptor beta (ER beta) in competitive binding assay B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2004) 14: 1417-1421 [PMID:15006374]
ChEMBL Inhibition of binding to recombinant human estrogen receptor beta B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2005) 15: 107-113 [PMID:15582421]
ChEMBL Binding potency for human ER beta B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2004) 14: 3861-3864 [PMID:15225685]
ChEMBL Binding affinity towards human estrogen receptor beta (ERbeta) B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2004) 14: 2551-2554 [PMID:15109649]
ChEMBL Inhibition of binding to recombinant human ERbeta by scintillation proximity assay B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2005) 15: 5124-5128 [PMID:16203138]
ChEMBL Inhibition of fluormone ES2 binding to estrogen receptor beta after 1 hr by fluorescence polarization assay B 8.09 pIC50 8.2 nM IC50 J Med Chem (2009) 52: 7544-7569 [PMID:19366247]
ChEMBL Binding affinity to ERbeta B 8.09 pIC50 8.2 nM IC50 J Med Chem (2006) 49: 3056-3059 [PMID:16722623]
ChEMBL Antagonist activity at human wild type ERbeta expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay F 8.16 pIC50 6.9 nM IC50 Bioorg Med Chem Lett (2010) 20: 5258-5261 [PMID:20659801]
ChEMBL Inhibition of human estrogen receptor 2 using tritiated estradiol incubated for 3 hr B 8.72 pIC50 1.9 nM IC50 Bioorg Med Chem Lett (2005) 15: 3912-3916 [PMID:15993065]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor beta B 8.8 pIC50 1.6 nM IC50 Bioorg Med Chem Lett (2005) 15: 2891-2893 [PMID:15911274]
ChEMBL Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor beta. B 6.59 pEC50 260 nM EC50 J Med Chem (2002) 45: 1399-1401 [PMID:11906280]
Estrogen receptor-β/Estrogen receptor beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3021] [GtoPdb: 621] [UniProtKB: Q62986]
ChEMBL Binding to Estrogen receptor- beta (ER beta) receptor B 6.33 pIC50 470 nM IC50 Bioorg Med Chem Lett (2002) 12: 2875-2878 [PMID:12270167]
ChEMBL Binding affinity foor Rat Estrogen receptor-beta B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2003) 13: 479-483 [PMID:12565955]
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 6.19 pKi 641 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.8 pIC50 1602 nM IC50 DrugMatrix in vitro pharmacology data
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL Inhibition of KDM1A (unknown origin) B 5.68 pIC50 2080 nM IC50 Eur J Med Chem (2022) 231: 114143-114143 [PMID:35101649]
ChEMBL Inhibition of LSD1 (unknown origin) B 5.68 pIC50 2080 nM IC50 Eur J Med Chem (2022) 228: 114042-114042 [PMID:34915312]
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 6.32 pKi 477 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.93 pIC50 1176 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 5.88 pKi 1330 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.4 pIC50 3989 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 6.55 pKi 280 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.55 pIC50 282 nM IC50 DrugMatrix in vitro pharmacology data
PLD1/Phospholipase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2536] [GtoPdb: 1433] [UniProtKB: Q13393]
ChEMBL Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis B 5.07 pIC50 8500 nM IC50 Nat Chem Biol (2009) 5: 108-117 [PMID:19136975]
ChEMBL Inhibition of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay B 5.37 pIC50 4300 nM IC50 Nat Chem Biol (2009) 5: 108-117 [PMID:19136975]
ChEMBL Inhibition of human PLD1b B 5.4 pIC50 4000 nM IC50 Nat Chem Biol (2009) 5: 108-117 [PMID:19136975]
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]
PLD2/Phospholipase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2734] [GtoPdb: 1434] [UniProtKB: O14939]
ChEMBL Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis B 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 108-117 [PMID:19136975]
ChEMBL Inhibition of human PLD2 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay B 5.47 pIC50 3400 nM IC50 Nat Chem Biol (2009) 5: 108-117 [PMID:19136975]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay B 4.93 pEC50 11710 nM EC50 Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Antagonist activity at progesterone receptor in human MCF7 cells B 7 pIC50 >100 nM IC50 Eur J Med Chem (2022) 227: 113869-113869 [PMID:34710747]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 6.07 pKi 846 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 5.73 pIC50 1861 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 6.38 pKi 414 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.84 pIC50 1450 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 6.65 pKi 226 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting B 7.16 pKi 69 nM Ki J Med Chem (2010) 53: 7573-7586 [PMID:20958049]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.45 pIC50 355 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 6.21 pKi 617 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.93 pIC50 1178 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 Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting B 6.12 pKi 750 nM Ki J Med Chem (2012) 55: 5704-5719 [PMID:22537153]
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 5.72 pKi 1900 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.45 pIC50 3576 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 DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.54 pKi 286 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 7.42 pKi 38 nM Ki J Med Chem (2005) 48: 4754-4764 [PMID:16033255]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.17 pIC50 681 nM IC50 DrugMatrix in vitro pharmacology data
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 5.44 pIC50 3666 nM IC50 DrugMatrix in vitro pharmacology data
GPER in Human [GtoPdb: 221] [UniProtKB: Q99527]
GtoPdb - - 7 pKi - - - Obstet Gynecol Int (2013) 2013: 472720 [PMID:24379833]

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]