ropsacitinib [Ligand Id: 11613] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4459585 (Pf-06826647, PF-06826647, Ropsacitinib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301390] [GtoPdb: 2048, 2047, 2269] [UniProtKB: O60674, P23458, P29597] | ||||||||
| ChEMBL | Inhibition of TYK2/JAK1/JAK2 signaling pathway in human whole blood spiked with CD3 +ve cells assessed as reduction in IL-6 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-6 addition and measured measured after 15 mins by immunostaining based FACS assay | B | 5.36 | pIC50 | 4370 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| ChEMBL | Inhibition of TYK2/JAK1/JAK2 signaling pathway in human whole blood spiked with CD3 +ve cells assessed as reduction in IL-6 induced STAT1 phosphorylation preincubated for 45 mins followed by IL-6 addition and measured measured after 15 mins by immunostaining based FACS assay | B | 6.25 | pIC50 | 566 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 6.42 | pIC50 | 383 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| ChEMBL | Inhibition of TYK2/JAK1/JAK2 signaling pathway in human lymphocytes of whole blood assessed as reduction in IL-27 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-27 addition and measured measured after 15 mins by FACS assay | B | 6.7 | pIC50 | 201 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 2047, 2269] [UniProtKB: P23458, P29597] | ||||||||
| ChEMBL | Inhibition of JAK1/TYK2 signaling pathway in human whole blood lymphocytes assessed as reduction in IL-10 induced STAT3 phosphorylation preincubated for 45 mins followed by IFN-alpha addition and measured measured after 15 mins by FACS assay | B | 6.37 | pIC50 | 427 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 6.42 | pIC50 | 383 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| ChEMBL | Inhibition of JAK1/TYK2 signaling pathway in human whole blood lymphocytes assessed as reduction in IFN-alpha induced STAT3 phosphorylation preincubated for 45 mins followed by IFN-alpha addition and measured measured after 15 mins by FACS assay | B | 7.18 | pIC50 | 66 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| ChEMBL | Inhibition of JAK1/TYK2 signaling pathway in human whole blood assessed as reduction in IL-12 induced STAT4 phosphorylation preincubated for 45 mins followed by IL-12 addition and measured measured after 15 mins by immunostaining based FACS assay | B | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 2048, 2269] [UniProtKB: O60674, P29597] | ||||||||
| ChEMBL | Inhibition of JAK2/TYK2 signaling pathway in human whole blood lymphocytes assessed as reduction in IL-23 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-23 addition and measured measured after 15 mins by immunostaining based FACS assay | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of recombinant human GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system using FITC-KGGEEEEYFELVKK as substrate in presence of ATP at Km by microfluidic assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Inhibition of recombinant human TYK2 JH1 kinase domain using 5FAM-KKSRGDYMTMQID as substrate incubated for 135 mins by caliper method | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2019) 62: 8973-8995 [PMID:31318208] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| ChEMBL | Inhibition of recombinant human His-tagged TYK2 expressed in baculovirus infected Sf21 cells using 5FAM-KKSRGDYMTMQID as substrate in presence of ATP at Km by microfluidic assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
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]
