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 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of JAK1 JH1 domain (unknown origin) in presence of 1 mM of ATP | B | 6.42 | pIC50 | 383 | nM | IC50 | J Med Chem (2023) 66: 10473-10496 [PMID:37427891] |
| GtoPdb | - | - | 6.42 | pIC50 | 383 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| GtoPdb | - | - | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2020) 63: 13561-13577 [PMID:32787094] |
| ChEMBL | Inhibition of JAK2 JH1 domain (unknown origin) in presence of 1 mM of ATP | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2023) 66: 10473-10496 [PMID:37427891] |
| 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] |
| ChEMBL | Inhibition of JAK3 JH1 domain (unknown origin) in presence of 1 mM of ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 10473-10496 [PMID:37427891] |
| 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] |
| ChEMBL | Inhibition of TYK2 JH1 domain (unknown origin) in presence of 1 mM of ATP | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2023) 66: 10473-10496 [PMID:37427891] |
| 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 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]
