Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T22939 | Target Info | |||
| Target Name | Progesterone receptor (PGR) | ||||
| Synonyms |
PR; Nuclear receptor subfamily 3 group C member 3; NR3C3
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| Target Type | Successful Target | ||||
| Gene Name | PGR | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Androgen receptor (AR) | Successful Target | ||||
| UniProt ID | ANDR_HUMAN | |||||
| Gene Name | AR | |||||
| Synonyms |
Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
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| Representative Drug(s) | Progesterone | Drug Info | Ki = 8.5 nM | Click to Show More | [1] | |
| 2 | BAY 86-5044 | Drug Info | IC50 = 54 nM | [7] | ||
| 3 | ONAPRISTONE | Drug Info | Ki ~ 100 nM | [3] | ||
| Co-Target Name | Mineralocorticoid receptor (MR) | Successful Target | ||||
| UniProt ID | MCR_HUMAN | |||||
| Gene Name | NR3C2 | |||||
| Synonyms |
Nuclear receptor subfamily 3 group C member 2; Mineralocorticoid receptor; MLR; MCR; Inner ear mineralocorticoid receptor; Delta
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| Representative Drug(s) | Progesterone | Drug Info | IC50 = 14 nM | Click to Show More | [2] | |
| 2 | ONAPRISTONE | Drug Info | IC50 = 470 nM | [4] | ||
| Co-Target Name | Estrogen receptor beta (ESR2) | Successful Target | ||||
| UniProt ID | ESR2_HUMAN | |||||
| Gene Name | ESR2 | |||||
| Synonyms |
Oestrogen receptor beta; Nuclear receptor subfamily 3 group A member 2; NR3A2; Erbeta; ESTRB; ER-beta; Beta-1
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| Representative Drug(s) | ONAPRISTONE | Drug Info | Ki < 20 nM | Click to Show More | [3] | |
| 2 | Progesterone | Drug Info | IC50 ~ 1000 nM | [2] | ||
| Co-Target Name | Glucocorticoid receptor (NR3C1) | Successful Target | ||||
| UniProt ID | GCR_HUMAN | |||||
| Gene Name | NR3C1 | |||||
| Synonyms |
Nuclear receptor subfamily 3 group C member 1; GRL; GR
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| Representative Drug(s) | ONAPRISTONE | Drug Info | IC50 = 27 nM | Click to Show More | [4] | |
| 2 | Progesterone | Drug Info | Ki = 30.5 nM | [5] | ||
| Co-Target Name | Corticosteroid-binding globulin (SERPINA6) | Successful Target | ||||
| UniProt ID | CBG_HUMAN | |||||
| Gene Name | SERPINA6 | |||||
| Synonyms |
Transcortin; SERPINA6; CBG
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| Representative Drug(s) | Progesterone | Drug Info | Ki = 41.69 nM | [6] | ||
| Co-Target Name | Opioid receptor sigma 1 (OPRS1) | Successful Target | ||||
| UniProt ID | SGMR1_HUMAN | |||||
| Gene Name | SIGMAR1 | |||||
| Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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| Representative Drug(s) | Progesterone | Drug Info | Ki = 260 nM | [8] | ||
| Co-Target Name | Estrogen receptor (ESR) | Successful Target | ||||
| UniProt ID | ESR1_HUMAN | |||||
| Gene Name | ESR1 | |||||
| Synonyms |
Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER
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| Representative Drug(s) | Progesterone | Drug Info | IC50 ~ 1000 nM | [9] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. J Med Chem. 1998 Oct 22;41(22):4354-9. | ||||
| REF 2 | Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators. Bioorg Med Chem Lett. 2003 Jun 16;13(12):2071-4. | ||||
| REF 3 | Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether. J Med Chem. 1996 Apr 26;39(9):1778-89. | ||||
| REF 4 | Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8. | ||||
| REF 5 | 5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification. J Med Chem. 1999 Apr 22;42(8):1466-72. | ||||
| REF 6 | Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR. J Med Chem. 2004 May 20;47(11):2732-42. | ||||
| REF 7 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6. | ||||
| REF 8 | Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. J Med Chem. 2005 Jul 28;48(15):4754-64. | ||||
| REF 9 | Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative ... J Med Chem. 2005 May 19;48(10):3463-6. | ||||
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