tamoxifen
One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.
Ligand Summary
UNII: 094ZI81Y45
PubChem: 2733526
Guide to Pharmacology: 1016
ChEMBL: CHEMBL83
DrugCentral: 2561
LyCHI: 77VBQQV883JS
Target Activities
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10
1 – 10 of 10
ESR1
Estrogen receptor
13 Activities
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1 – 10 of 13
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7 | Bioorg. Med. Chem. Lett., (2009) 19:4:1218 | ||||
IC50 | 7.16 | Bioorg. Med. Chem., (2008) 16:21:9554 | ||||
IC50 | 7.21 | J. Med. Chem., (2014) 57:22:9370 | ||||
IC50 | 7.21 | J. Med. Chem., (2014) 57:22:9370 | ||||
IC50 | 7.38 | J. Med. Chem., (1999) 42:16:3126 | ||||
IC50 | 7.41 | J. Med. Chem., (2013) 56:14:5782 | ||||
Ki | 7.51 | Bioorg. Med. Chem., (2010) 18:15:5593 | ||||
IC50 | 7.61 | J. Med. Chem., (2015) 58:20:8128 | ||||
IC50 | 8.08 | Bioorg. Med. Chem. Lett., (2002) 12:9:1283 | ||||
IC50 | 8.1 | Eur. J. Med. Chem., (2016) 112:None:171 | ||||
ESR2
Estrogen receptor beta
3 Activities
SIGMAR1
Sigma non-opioid intracellular receptor 1
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.46 | J. Med. Chem., (2005) 48:15:4754 | ||||
IC50 | 7.68 | None, None:None:None | ||||
Ki | 8.06 | None, None:None:None | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.8 | Eur. J. Med. Chem., (2011) 46:2:618 | ||||
IC50 | 6.01 | None, None:None:None | ||||
Ki | 6.1 | None, None:None:None | ||||
EBPL
Emopamil-binding protein-like
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.55 | Bioorg. Med. Chem., (2013) 21:1:215 | ||||
Ki | 8.55 | |||||
EBP
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.3 | J. Med. Chem., (2005) 48:15:4754 | ||||
Kd | 9 | |||||
ABCB1
Multidrug resistance protein 1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7 | J. Med. Chem., (2002) 45:26:5671 | ||||
TBXAS1
Thromboxane-A synthase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.04 | None, None:None:None | ||||
GPER1
G-protein coupled estrogen receptor 1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6 | ||||||
DHCR7
7-dehydrocholesterol reductase
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 9 | |||||