Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T18226 | Target Info | |||
| Target Name | HUMAN clathrin-mediated endocytosis (RME) | ||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Dopamine D2 receptor (D2R) | Successful Target | ||||
| UniProt ID | DRD2_HUMAN | |||||
| Gene Name | DRD2 | |||||
| Synonyms |
Dopamine receptor 2; D(2) dopamine receptor
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| Representative Drug(s) | Chlorpromazine | Drug Info | IC50 = 1 nM | [1] | ||
| Co-Target Name | Dopamine D3 receptor (D3R) | Successful Target | ||||
| UniProt ID | DRD3_HUMAN | |||||
| Gene Name | DRD3 | |||||
| Synonyms |
D(3) dopamine receptor
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 1.585 nM | [2] | ||
| Co-Target Name | 5-HT 2A receptor (HTR2A) | Successful Target | ||||
| UniProt ID | 5HT2A_HUMAN | |||||
| Gene Name | HTR2A | |||||
| Synonyms |
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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| Representative Drug(s) | Chlorpromazine | Drug Info | IC50 = 3.4 nM | [3] | ||
| Co-Target Name | Histamine H1 receptor (H1R) | Successful Target | ||||
| UniProt ID | HRH1_HUMAN | |||||
| Gene Name | HRH1 | |||||
| Synonyms |
HH1R; H1R
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 4.25 nM | [4] | ||
| Co-Target Name | Dopamine D4 receptor (D4R) | Successful Target | ||||
| UniProt ID | DRD4_HUMAN | |||||
| Gene Name | DRD4 | |||||
| Synonyms |
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 25.12 nM | [2] | ||
| Co-Target Name | 5-HT 2C receptor (HTR2C) | Successful Target | ||||
| UniProt ID | 5HT2C_HUMAN | |||||
| Gene Name | HTR2C | |||||
| Synonyms |
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 27 nM | [5] | ||
| Co-Target Name | 5-HT 2B receptor (HTR2B) | Successful Target | ||||
| UniProt ID | 5HT2B_HUMAN | |||||
| Gene Name | HTR2B | |||||
| Synonyms |
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 39.81 nM | [2] | ||
| Co-Target Name | Serotonin transporter (SERT) | Successful Target | ||||
| UniProt ID | SC6A4_HUMAN | |||||
| Gene Name | SLC6A4 | |||||
| Synonyms |
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 63.1 nM | [2] | ||
| Co-Target Name | Dopamine D1 receptor (D1R) | Successful Target | ||||
| UniProt ID | DRD1_HUMAN | |||||
| Gene Name | DRD1 | |||||
| Synonyms |
D(1A) dopamine receptor
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 96 nM | [4] | ||
| Co-Target Name | Muscarinic acetylcholine receptor M1 (CHRM1) | Successful Target | ||||
| UniProt ID | ACM1_HUMAN | |||||
| Gene Name | CHRM1 | |||||
| Synonyms |
M1 receptor
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 125.89 nM | [2] | ||
| Co-Target Name | Muscarinic acetylcholine receptor M4 (CHRM4) | Successful Target | ||||
| UniProt ID | ACM4_HUMAN | |||||
| Gene Name | CHRM4 | |||||
| Synonyms |
M4 receptor; CHRM4
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 158.49 nM | [2] | ||
| Co-Target Name | Dopamine D5 receptor (D5R) | Successful Target | ||||
| UniProt ID | DRD5_HUMAN | |||||
| Gene Name | DRD5 | |||||
| Synonyms |
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 172 nM | [4] | ||
| Co-Target Name | Aldehyde oxidase (AOX1) | Successful Target | ||||
| UniProt ID | AOXA_HUMAN | |||||
| Gene Name | AOX1 | |||||
| Synonyms |
AOX1
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| Representative Drug(s) | Chlorpromazine | Drug Info | IC50 = 570 nM | [6] | ||
| Co-Target Name | Multidrug resistance protein 1 (ABCB1) | Clinical trial Target | ||||
| UniProt ID | MDR1_HUMAN | |||||
| Gene Name | ABCB1 | |||||
| Synonyms |
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 600 nM | [7] | ||
| Co-Target Name | 5-HT 1A receptor (HTR1A) | Successful Target | ||||
| UniProt ID | 5HT1A_HUMAN | |||||
| Gene Name | HTR1A | |||||
| Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 673 nM | [8] | ||
| Co-Target Name | 5-HT 6 receptor (HTR6) | Clinical trial Target | ||||
| UniProt ID | 5HT6R_HUMAN | |||||
| Gene Name | HTR6 | |||||
| Synonyms |
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 4 nM | [9] | ||
| Co-Target Name | 5-HT 7 receptor (HTR7) | Clinical trial Target | ||||
| UniProt ID | 5HT7R_HUMAN | |||||
| Gene Name | HTR7 | |||||
| Synonyms |
Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki = 10.72 nM | [10] | ||
| Co-Target Name | Histamine H3 receptor (H3R) | Clinical trial Target | ||||
| UniProt ID | HRH3_HUMAN | |||||
| Gene Name | HRH3 | |||||
| Synonyms |
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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| Representative Drug(s) | Chlorpromazine | Drug Info | Ki ~ 1000 nM | [4] | ||
| Co-Target Name | Glutamate [NMDA] receptor | Co-Target | ||||
| UniProt ID | NMDE1_HUMAN; NMDE2_HUMAN; NMDE3_HUMAN; NMD3A_HUMAN; NMD3B_HUMAN; NMDE4_HUMAN; NMDZ1_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | Chlorpromazine | Drug Info | IC50 = 600 nM | [11] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. Eur J Med Chem. 2015 Mar 6;92:221-35. | ||||
| REF 2 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. J Med Chem. 2007 Oct 18;50(21):5103-8. | ||||
| REF 3 | Polypharmacology-foe or friend? J Med Chem. 2013 Nov 27;56(22):8955-71. | ||||
| REF 4 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42. | ||||
| REF 5 | CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. Bioorg Med Chem. 2011 Oct 1;19(19):5756-62. | ||||
| REF 6 | Aldehyde oxidase: an enzyme of emerging importance in drug discovery. J Med Chem. 2010 Dec 23;53(24):8441-60. | ||||
| REF 7 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). J Med Chem. 2002 Dec 19;45(26):5671-86. | ||||
| REF 8 | Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives. J Med Chem. 1993 Apr 16;36(8):1053-68. | ||||
| REF 9 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812. | ||||
| REF 10 | Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor. Bioorg Med Chem. 2013 May 1;21(9):2568-76. | ||||
| REF 11 | Synthesis and evaluation of 3-substituted 17-methylmorphinan analogs as potential anticonvulsant agents. J Med Chem. 1992 Oct 30;35(22):4135-42. | ||||
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