raloxifene
A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
Ligand Summary
UNII: YX9162EO3I
PubChem: 25010765
PubChem: 5035
Guide to Pharmacology: 2820
ChEMBL: CHEMBL81
ChEMBL: CHEMBL1116
DrugCentral: 2351
LyCHI: Z21APBSNPM3W
Target Activities
Items per page:
10
1 – 8 of 8
ESR1
Estrogen receptor
36 Activities
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1 – 10 of 36
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.66 | J. Med. Chem., (2003) 46:14:2945 | ||||
EC50 | 7.66 | J. Med. Chem., (2008) 51:13:3661 | ||||
EC50 | 7.66 | J. Med. Chem., (2002) 45:7:1399 | ||||
IC50 | 7.66 | J. Med. Chem., (2005) 48:2:364 | ||||
IC50 | 7.69 | J. Med. Chem., (2007) 50:11:2682 | ||||
IC50 | 8.15 | Bioorg. Med. Chem. Lett., (2003) 13:11:1919 | ||||
IC50 | 8.4 | J. Med. Chem., (2001) 44:11:1654 | ||||
IC50 | 8.62 | J. Med. Chem., (2003) 46:14:2945 | ||||
IC50 | 8.62 | J. Med. Chem., (2005) 48:2:364 | ||||
IC50 | 8.7 | Bioorg. Med. Chem. Lett., (2000) 10:2:147 | ||||
ESR2
Estrogen receptor beta
24 Activities
Items per page:
1 – 10 of 24
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.37 | Bioorg. Med. Chem. Lett., (2000) 10:2:147 | ||||
IC50 | 7.37 | J. Med. Chem., (2001) 44:11:1654 | ||||
Ki | 7.64 | Bioorg. Med. Chem. Lett., (2008) 18:18:5075 | ||||
IC50 | 7.72 | Bioorg. Med. Chem. Lett., (2005) 15:5:1505 | ||||
IC50 | 7.82 | J. Med. Chem., (2002) 45:25:5492 | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2005) 15:23:5124 | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2003) 13:3:479 | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2004) 14:6:1417 | ||||
IC50 | 7.92 | J. Med. Chem., (2004) 47:9:2171 | ||||
IC50 | 7.92 | Bioorg. Med. Chem. Lett., (2004) 14:10:2551 | ||||
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) | ||
|---|---|---|---|---|---|---|
IC50 | 6.17 | None, None:None:None | ||||
Ki | 6.54 | None, None:None:None | ||||
Ki | 7.42 | J. Med. Chem., (2005) 48:15:4754 | ||||
SLC6A2
Sodium-dependent noradrenaline transporter
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.55 | None, None:None:None | ||||
Ki | 6.55 | None, None:None:None | ||||
ACHE
Acetylcholinesterase
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 | 6.4 | None, None:None:None | ||||
EBP
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
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 | 9 | J. Med. Chem., (2005) 48:15:4754 | ||||
HTR2B
5-hydroxytryptamine receptor 2B
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.16 | J. Med. Chem., (2010) 53:21:7573 | ||||
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) | ||
|---|---|---|---|---|---|---|
- | 7 | |||||