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ChEMBL ligand: CHEMBL1628706 (CP-481715) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246] | ||||||||
GtoPdb | - | - | 8 | pKd | 9.2 | nM | Kd | J Biol Chem (2003) 278: 40473-80 [PMID:12909630] |
ChEMBL | Binding affinity to CCR1 | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
ChEMBL | Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay | F | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 435-440 [PMID:30455146] |
ChEMBL | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay | B | 7.41 | pIC50 | 39 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 435-440 [PMID:30455146] |
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] | ||||||||
ChEMBL | Binding affinity to CCR5 | B | 7.18 | pKi | 66 | nM | Ki | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Binding affinity to muscarinic M2 receptor | B | 5.88 | pKi | 1323 | nM | Ki | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
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]