solcitinib [Ligand Id: 9697] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3301606 (G-154578, G154578, Glpg-0778, GLPG-0778, GLPG0778, GLPG-0788, Gsk-2586184, GSK-2586184, GSK-2586184A, GSK2586184A, Solcitinib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of JAK1 (unknown origin) | B | 8.01 | pIC50 | 9.8 | nM | IC50 | Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325] |
| GtoPdb | - | - | 8.18 | pIC50 | 6.6 | nM | IC50 | WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010) |
| ChEMBL | Inhibition Assay: Recombinant human JAK1 (catalytic domain, amino acids 866-1154; catalog number PV4774) was purchased from Invitrogen. 1 ng of JAK1 was incubated with 20 nM Ulight-JAK1(tyr1023) peptide (Perkin Elmer catalog number TRF0121) in kinase reaction buffer (25 mM MOPS pH6.8, 0.016% Brij-35, 8.33 mM MgCl2, 3.33 mM DTT, 7 uM ATP) with or without 4 uL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 20 uL, in a white 384 Luminotrac 200 plate (Greiner, catalog number 781075). After 60 min at room temperature, reactions were stopped by adding 20 uL/well of detection mixture (1x detection buffer (Perkin Elmer, catalog number CR97-100C), 0.5 nM Europium-anti-phosphotyrosine (PT66) (Perkin Elmer, catalog number AD0068), 10 mM EDTA). Readout is performed using the Envision with excitation at 320 nm and measuring emission at 615 nm (Perkin Elmer). Kinase activity was calculated by subtracting relative fluorescence units (RFU). | B | 8.18 | pIC50 | 6.6 | nM | IC50 | US-8796457-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2014) |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 (unknown origin) | B | 6.97 | pIC50 | 107.8 | nM | IC50 | Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325] |
| GtoPdb | - | - | 7.17 | pIC50 | 67 | nM | IC50 | WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010) |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of JAK3 (unknown origin) | B | 6.27 | pIC50 | 539 | nM | IC50 | Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325] |
| GtoPdb | - | - | 6.39 | pIC50 | 408 | nM | IC50 | WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010) |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Inhibition of TYK2 (unknown origin) | B | 6.65 | pIC50 | 225 | nM | IC50 | Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325] |
| GtoPdb | - | - | 6.66 | pIC50 | 219 | nM | IC50 | WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010) |
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]
