Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T52790 | Target Info | |||
Target Name | Substance-K receptor (TACR2) | ||||
Synonyms |
Tachykinin receptor 2; Tachykinin neurokinin 2 receptor; TACR2; SKR; Neurokinin A receptor; NK-2R; NK-2 receptor
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Target Type | Clinical trial Target | ||||
Gene Name | TACR2 | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Melanocortin receptor 4 (MC4R) | Successful Target | ||||
UniProt ID | MC4R_HUMAN | |||||
Gene Name | MC4R | |||||
Synonyms |
MC4-R
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Representative Drug(s) | PMX-53 | Drug Info | IC50 = 400 nM | [1] | ||
Co-Target Name | Vasopressin V1a receptor (V1AR) | Successful Target | ||||
UniProt ID | V1AR_HUMAN | |||||
Gene Name | AVPR1A | |||||
Synonyms |
Vascular/hepatic-type arginine vasopressin receptor; V1aR; V1a vasopressin receptor; Antidiuretic hormone receptor 1a; AVPR1; AVPR V1a
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Representative Drug(s) | PMX-53 | Drug Info | IC50 = 740 nM | [1] | ||
Co-Target Name | Cytochrome P450 26 (CYP26A1) | Clinical trial Target | ||||
UniProt ID | CP26A_HUMAN | |||||
Gene Name | CYP26A1 | |||||
Synonyms |
Retinoic acid-metabolizing cytochrome; Retinoic acid inducible enzyme; Retinoic acid 4-hydroxylase; P450RAI; P450 retinoic acid-inactivating 1; HP450RAI; Cytochrome P450RAI; CYP26A1
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Representative Drug(s) | Rambazole | Drug Info | IC50 = 5.1 nM | [2] | ||
Co-Target Name | C5a anaphylatoxin chemotactic receptor (C5AR1) | Successful Target | ||||
UniProt ID | C5AR1_HUMAN | |||||
Gene Name | C5AR1 | |||||
Synonyms |
CD88; C5aR; C5a-R; C5a anaphylatoxin chemotactic receptor 1; C5R1
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Representative Drug(s) | PMX-53 | Drug Info | IC50 = 15 nM | [3] | ||
Co-Target Name | Cytochrome P450 26B1 (CYP26B1) | Co-Target | ||||
UniProt ID | CP26B_HUMAN | |||||
Gene Name | CYP26B1 | |||||
Synonyms |
Cytochrome P450 26A2; Cytochrome P450 retinoic acid-inactivating 2; Cytochrome P450RAI-2; Retinoic acid-metabolizing cytochrome
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Representative Drug(s) | Rambazole | Drug Info | IC50 = 0.46 nM | [2] |
References | Top | ||||
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REF 1 | Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. | ||||
REF 2 | Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase. J Med Chem. 2016 Mar 24;59(6):2579-95. | ||||
REF 3 | Selective hexapeptide agonists and antagonists for human complement C3a receptor. J Med Chem. 2010 Jul 8;53(13):4938-48. |
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