Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T52921 | Target Info | |||
| Target Name | Nociceptin receptor (OPRL1) | ||||
| Synonyms |
Orphanin FQ receptor; Opioid-receptor-like 1; Opioid receptor like-1 receptor; Opioid receptor 4; ORL-1 receptor; ORL-1; OPRL1; OP(4); Kappa-type 3 opioid receptor; KOR-3
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| Target Type | Clinical trial Target | ||||
| Gene Name | OPRL1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Opioid receptor kappa (OPRK1) | Successful Target | ||||
| UniProt ID | OPRK_HUMAN | |||||
| Gene Name | OPRK1 | |||||
| Synonyms |
OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1
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| Representative Drug(s) | NOCICEPTIN | Drug Info | EC50 = 78.5 nM | [1] | ||
| Co-Target Name | Opioid receptor mu (MOP) | Successful Target | ||||
| UniProt ID | OPRM_HUMAN | |||||
| Gene Name | OPRM1 | |||||
| Synonyms |
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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| Representative Drug(s) | NOCICEPTIN | Drug Info | Ki = 270 nM | [2] | ||
| 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 | [3] | ||
| 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 | [3] | ||
| Co-Target Name | Opioid receptor delta (OPRD1) | Successful Target | ||||
| UniProt ID | OPRD_HUMAN | |||||
| Gene Name | OPRD1 | |||||
| Synonyms |
OPRD; Delta-type opioid receptor; Delta opioid receptor; DOR-1; D-OR-1
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| Representative Drug(s) | NOCICEPTIN | Drug Info | Ki ~ 1000 nM | [4] | ||
| 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 | [5] | ||
| Co-Target Name | Substance-K receptor (TACR2) | Clinical trial Target | ||||
| UniProt ID | NK2R_HUMAN | |||||
| Gene Name | TACR2 | |||||
| Synonyms |
Tachykinin receptor 2; Tachykinin neurokinin 2 receptor; TACR2; SKR; Neurokinin A receptor; NK-2R; NK-2 receptor
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| Representative Drug(s) | PMX-53 | Drug Info | IC50 = 87 nM | [3] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. J Med Chem. 2011 Oct 13;54(19):6531-7. | ||||
| REF 2 | Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist. J Med Chem. 2002 Nov 21;45(24):5353-7. | ||||
| REF 3 | 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 4 | Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug. J Med Chem. 2009 Feb 12;52(3):610-25. | ||||
| REF 5 | Selective hexapeptide agonists and antagonists for human complement C3a receptor. J Med Chem. 2010 Jul 8;53(13):4938-48. | ||||
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