ATC0175 [Ligand Id: 1305] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL182150 (ATC-0175)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
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  • Y5 receptor/Neuropeptide Y receptor type 5 in Human [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Displacement of [3H]prazosin from human adrenergic alpha1A receptor B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibitory activity against alpha-2A adrenergic receptor by using [3H]MK-912 as radioligand expressed in COS-1 cells B 6.59 pIC50 260 nM IC50 Bioorg Med Chem Lett (2005) 15: 3853-3856 [PMID:16002290]
ChEMBL Displacement of [3H]MK-912 from human adrenergic alpha2A receptor B 6.98 pIC50 104 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]pyrilamine from human histamine H1 receptor B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
ChEMBL Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay B 8.08 pIC50 8.28 nM IC50 Bioorg Med Chem Lett (2019) 29: 126741-126741 [PMID:31678007]
GtoPdb - - 8.1 pIC50 7.23 nM IC50 J Pharmacol Exp Ther (2005) 313: 831-839 [PMID:15677346]
ChEMBL Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay F 8.14 pIC50 7.2 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]
ChEMBL Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2005) 15: 3853-3856 [PMID:16002290]
Y5 receptor/Neuropeptide Y receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4561] [GtoPdb: 308] [UniProtKB: Q15761]
ChEMBL Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells B 5.57 pIC50 2700 nM IC50 Bioorg Med Chem Lett (2005) 15: 3853-3856 [PMID:16002290]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibition of human 5HT1A B 7.77 pIC50 16.9 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]rauwolsine from human 5HT2B receptor B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]
ChEMBL Displacement of [125I]LSD from human 5HT2B receptor B 8.02 pIC50 9.66 nM IC50 Bioorg Med Chem Lett (2009) 19: 6166-6171 [PMID:19773162]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]