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Assay Detail

CHEMBL859670

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Functional
Inhibition of LPS-induced IL1-beta production in human whole blood
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.
Goldstein DM, Alfredson T, Bertrand J, Browner MF, Clifford K, Dalrymple SA, Dunn J, Freire-Moar J, Harris S, Labadie SS, La Fargue J, Lapierre JM, Larrabee S, Li F, Papp E, McWeeney D, Ramesha C, Roberts R, Rotstein D, San Pablo B, Sjogren EB, So OY, Talamas FX, Tao W, Trejo A, Villasenor A, Welch M, Welch T, Weller P, Whiteley PE, Young K, Zipfel S.
J Med Chem (2006) 49 : 1562 -1575
PubMed 16509574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.99 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202851 1 6.66
CHEMBL203567 RO-3201195 1.0 1 6.24
CHEMBL380849 1 6.16
CHEMBL205133 1 6.12
CHEMBL438628 1 6.04
CHEMBL203508 1 5.92
CHEMBL380850 1 5.44
CHEMBL203908 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202851 IC50 = 220.0 nM 6.66
CHEMBL203567 RO-3201195 IC50 = 570.0 nM 6.24
CHEMBL380849 IC50 = 690.0 nM 6.16
CHEMBL205133 IC50 = 760.0 nM 6.12
CHEMBL438628 IC50 = 920.0 nM 6.04
CHEMBL203508 IC50 = 1200.0 nM 5.92
CHEMBL380850 IC50 = 3600.0 nM 5.44
CHEMBL203908 IC50 = 4640.0 nM 5.33