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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]