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
Target Activities
ESR1
Estrogen receptor
19 Activities
Items per page:
1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 7.82 | |||||
- | 7.8 | |||||
IC50 | 8.82 | Eur J Med Chem, (2019) 166:None:281 | ||||
IC50 | 8.1 | Eur. J. Med. Chem., (2016) 112:None:171 | ||||
IC50 | 8.08 | Bioorg. Med. Chem. Lett., (2002) 12:9:1283 | ||||
IC50 | 7.61 | J. Med. Chem., (2015) 58:20:8128 | ||||
Ki | 7.51 | Bioorg. Med. Chem., (2010) 18:15:5593 | ||||
IC50 | 7.41 | J. Med. Chem., (2013) 56:14:5782 | ||||
IC50 | 7.38 | J. Med. Chem., (1999) 42:16:3126 | ||||
IC50 | 7.21 | J. Med. Chem., (2014) 57:22:9370 | ||||
ESR2
Estrogen receptor beta
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
7.16 | ||||||
7.17 | ||||||
Ki | 9.29 | ACS Med. Chem. Lett., (2012) 3:3:207 | ||||
IC50 | 8.3 | J Med Chem, (2019) 62:14:6525 | ||||
IC50 | 7.1 | Bioorg Med Chem, (2017) 25:20:5216 | ||||
SIGMAR1
Sigma non-opioid intracellular receptor 1
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.06 | None, None:None:None | ||||
IC50 | 7.68 | None, None:None:None | ||||
Ki | 7.46 | J. Med. Chem., (2005) 48:15:4754 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.1 | None, None:None:None | ||||
IC50 | 6.01 | None, None:None:None | ||||
IC50 | 5.8 | Eur. J. Med. Chem., (2011) 46:2:618 | ||||
EBP
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
2 Activities
Items per page:
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 | |||||
EBPL
Emopamil-binding protein-like
2 Activities
Items per page:
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 | |||||
GPER1
G-protein coupled estrogen receptor 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
6 | ||||||
TBXAS1
Thromboxane-A synthase
1 Activities
Items per page:
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 | ||||
CYP3A4
Cytochrome P450 3A4
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.7 | Curr. Drug Metab., (2005) 6:1:413 | ||||
ESRRG
Estrogen-related receptor gamma
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.21 | Bioorg Med Chem, (2017) 25:20:5216 | ||||
ABCB1
Multidrug resistance protein 1
1 Activities
Items per page:
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 | ||||
CYP2B6
Cytochrome P450 2B6
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.05 | Curr. Drug Metab., (2005) 6:1:413 | ||||
DHCR7
7-dehydrocholesterol reductase
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 9 | |||||