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Assay Detail

CHEMBL3825641

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of p38alpha (unknown origin)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus R, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, Beal AM, Finger JN, Cook MN, King BW, Ouellette MT, Totoritis RD, Pierdomenico M, Negroni A, Stronati L, Cucchiara S, Ziółkowski B, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Casillas LN.
J Med Chem (2016) 59 : 4867 -4880
PubMed 27109867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.75 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237347 GW559768X 1 6.30
CHEMBL3822938 1 5.97
CHEMBL237345 1 5.43
CHEMBL3823499 1 5.29
CHEMBL3823809 1 -
CHEMBL3822791 1 -
CHEMBL3822754 1 -
CHEMBL3822573 1 -
CHEMBL3824056 1 -
CHEMBL3823527 1 -
CHEMBL3822577 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237347 GW559768X IC50 = 500.0 nM 6.30
CHEMBL3822938 IC50 = 1080.0 nM 5.97
CHEMBL237345 IC50 = 3740.0 nM 5.43
CHEMBL3823499 IC50 = 5119.0 nM 5.29
CHEMBL3823809 IC50 > 5000.0 nM -
CHEMBL3822791 IC50 > 5000.0 nM -
CHEMBL3822754 IC50 > 5000.0 nM -
CHEMBL3822573 IC50 > 5000.0 nM -
CHEMBL3824056 IC50 > 5000.0 nM -
CHEMBL3823527 IC50 > 5000.0 nM -
CHEMBL3822577 IC50 > 5000.0 nM -