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ChEMBL ligand: CHEMBL3577945 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597] | ||||||||
ChEMBL | Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation | B | 8.33 | pIC50 | 4.7 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
GtoPdb | - | - | 9.15 | pIC50 | 0.7 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-44 [PMID:25893046] |
ChEMBL | Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature | B | 9.15 | pIC50 | 0.7 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
ChEMBL | Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins | B | 9.15 | pIC50 | 0.7 | nM | IC50 | ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130] |
ChEMBL | Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC | B | 9.62 | pIC50 | 0.24 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] | ||||||||
ChEMBL | Antagonist activity against CCR5 in whole blood (unknown origin) assessed as reduction in CD11b upregulation | B | 8.37 | pIC50 | 4.3 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
ChEMBL | Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs | B | 8.62 | pIC50 | 2.4 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
ChEMBL | Antagonist activity at CCR5 (unknown origin) expressed in human HT1080 cells assessed as blockade of MIP1beta-binding to receptor | B | 8.62 | pIC50 | 2.4 | nM | IC50 | ACS Med Chem Lett (2019) 10: 300-305 [PMID:30891130] |
GtoPdb | - | - | 8.62 | pIC50 | 2.4 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-44 [PMID:25893046] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG expressed in HEK293 cells assessed as reduction in peak tail current at holding potential of 80 mV to +20 mV by whole cell patch clamp assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Inhibition of muscarinic acetylcholine receptor M1 (unknown origin) | B | 6.47 | pKi | 341 | nM | Ki | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Inhibition of muscarinic acetylcholine receptor M2 (unknown origin) | B | 5.4 | pKi | 4010 | nM | Ki | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
ChEMBL | Inhibition of muscarinic acetylcholine receptor M4 (unknown origin) | B | 6.06 | pKi | 865 | nM | Ki | ACS Med Chem Lett (2015) 6: 439-444 [PMID:25893046] |
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]