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

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ChEMBL ligand: CHEMBL81 (Evista, J22.982B, LY-139481, Raloxifene)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • acetylcholinesterase (Cartwright 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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  • 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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  • 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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  • 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 (Cartwright 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
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]
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 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 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 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 to ERalpha B 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (2006) 49: 3056-3059 [PMID:16722623]
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 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