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: 5035
PubChem: 25010765
Guide to Pharmacology: 2820
ChEMBL: CHEMBL81
ChEMBL: CHEMBL1116
DrugCentral: 2351
LyCHI: Z21APBSNPM3W
Target Activities
ESR1
Estrogen receptor
45 Activities
Items per page:
1 – 10 of 45
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
- | 9.5 | |||||
- | 9.5 | |||||
Ki | 10.52 | J. Med. Chem., (2005) 48:19:5989 | ||||
Ki | 9.8 | None, None:None:None | ||||
IC50 | 9.74 | Bioorg Med Chem, (2019) 27:10:1952 | ||||
Ki | 9.66 | Bioorg. Med. Chem. Lett., (2001) 11:14:1939 | ||||
IC50 | 9.52 | Bioorg. Med. Chem. Lett., (2010) 20:17:5258 | ||||
Ki | 9.43 | ACS Med. Chem. Lett., (2012) 3:3:207 | ||||
Ki | 9.42 | ACS Med. Chem. Lett., (2012) 3:3:207 | ||||
Ki | 9.4 | Bioorg. Med. Chem. Lett., (2003) 13:11:1907 | ||||
ESR2
Estrogen receptor beta
26 Activities
Items per page:
1 – 10 of 26
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 8 | |||||
IC50 | 8.8 | Bioorg. Med. Chem. Lett., (2005) 15:11:2891 | ||||
IC50 | 8.72 | Bioorg. Med. Chem. Lett., (2005) 15:17:3912 | ||||
Ki | 8.56 | ACS Med. Chem. Lett., (2012) 3:3:207 | ||||
Ki | 8.37 | Bioorg. Med. Chem. Lett., (2003) 13:11:1907 | ||||
Ki | 8.37 | Bioorg. Med. Chem., (2016) 24:4:759 | ||||
Ki | 8.35 | J. Med. Chem., (2005) 48:19:5989 | ||||
IC50 | 8.16 | Bioorg. Med. Chem. Lett., (2010) 20:17:5258 | ||||
IC50 | 8.09 | J. Med. Chem., (2006) 49:11:3056 | ||||
IC50 | 8.09 | J. Med. Chem., (2009) 52:23:7544 | ||||
AOX1
Aldehyde oxidase
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 9.06 | Drug Metab. Dispos., (2013) 41:1:24 | ||||
Ki | 9.05 | J. Med. Chem., (2010) 53:24:8441 | ||||
Ki | 8.64 | Drug Metab. Dispos., (2013) 41:1:24 | ||||
IC50 | 8.52 | J. Med. Chem., (2010) 53:24:8441 | ||||
IC50 | 8.1 | J Agric Food Chem, (2011) 59:9:4860 | ||||
IC50 | 7.35 | None, None:None:None | ||||
IC50 | 7.35 | |||||
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 | 7.42 | J. Med. Chem., (2005) 48:15:4754 | ||||
Ki | 6.54 | None, None:None:None | ||||
IC50 | 6.17 | None, None:None:None | ||||
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 | ||||
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 | |||||
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 | ||||
ACHE
Acetylcholinesterase
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.4 | None, None:None:None | ||||
EBP
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase
1 Activities
Items per page:
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 | ||||
C5
Complement C5
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Kd | 6.15 | Bioorg Med Chem, (2019) 27:19:115052 | ||||