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ChEMBL ligand: CHEMBL182150 (ATC-0175) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]