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Assay Detail

CHEMBL859283

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Binding
Displacement of [33P] ATP from human recombinant active p38alpha
ChEMBL ↗
42
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 42 5.73 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278041 SB-202190 — 1 7.52
CHEMBL203926 — — 1 6.75
CHEMBL203908 — — 1 6.64
CHEMBL206187 — — 1 6.51
CHEMBL380755 — — 1 6.47
CHEMBL438628 — — 1 6.23
CHEMBL203567 RO-3201195 1.0 1 6.16
CHEMBL206339 — — 1 6.11
CHEMBL202851 — — 1 6.10
CHEMBL380849 — — 1 6.07
CHEMBL203978 — — 1 6.01
CHEMBL408417 — — 1 5.97
CHEMBL424677 — — 1 5.96
CHEMBL205133 — — 1 5.92
CHEMBL203770 — — 1 5.90
CHEMBL380850 — — 1 5.90
CHEMBL203344 — — 1 5.89
CHEMBL382175 — — 1 5.88
CHEMBL425401 — — 1 5.79
CHEMBL383844 — — 1 5.76
CHEMBL203932 — — 1 5.76
CHEMBL274506 — — 1 5.74
CHEMBL426122 — — 2 5.70
CHEMBL203133 — — 1 5.64
CHEMBL203333 — — 1 5.64
CHEMBL380531 — — 1 5.61
CHEMBL204345 — — 1 5.54
CHEMBL204600 — — 1 5.50
CHEMBL203508 — — 1 5.46
CHEMBL202737 — — 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278041 SB-202190 IC50 = 30.0 nM 7.52
CHEMBL203926 — IC50 = 180.0 nM 6.75
CHEMBL203908 — IC50 = 230.0 nM 6.64
CHEMBL206187 — IC50 = 310.0 nM 6.51
CHEMBL380755 — IC50 = 340.0 nM 6.47
CHEMBL438628 — IC50 = 590.0 nM 6.23
CHEMBL203567 RO-3201195 IC50 = 700.0 nM 6.16
CHEMBL206339 — IC50 = 780.0 nM 6.11
CHEMBL202851 — IC50 = 790.0 nM 6.10
CHEMBL380849 — IC50 = 850.0 nM 6.07
CHEMBL203978 — IC50 = 980.0 nM 6.01
CHEMBL408417 — IC50 = 1080.0 nM 5.97
CHEMBL424677 — IC50 = 1100.0 nM 5.96
CHEMBL205133 — IC50 = 1200.0 nM 5.92
CHEMBL203770 — IC50 = 1270.0 nM 5.90
CHEMBL380850 — IC50 = 1250.0 nM 5.90
CHEMBL203344 — IC50 = 1280.0 nM 5.89
CHEMBL382175 — IC50 = 1320.0 nM 5.88
CHEMBL425401 — IC50 = 1640.0 nM 5.79
CHEMBL383844 — IC50 = 1720.0 nM 5.76
CHEMBL203932 — IC50 = 1740.0 nM 5.76
CHEMBL274506 — IC50 = 1840.0 nM 5.74
CHEMBL426122 — IC50 = 2000.0 nM 5.70
CHEMBL203133 — IC50 = 2280.0 nM 5.64
CHEMBL203333 — IC50 = 2300.0 nM 5.64
CHEMBL380531 — IC50 = 2440.0 nM 5.61
CHEMBL426122 — IC50 = 2650.0 nM 5.58
CHEMBL204345 — IC50 = 2860.0 nM 5.54
CHEMBL204600 — IC50 = 3130.0 nM 5.50
CHEMBL203508 — IC50 = 3500.0 nM 5.46
CHEMBL202737 — IC50 = 4040.0 nM 5.39
CHEMBL203721 — IC50 = 4760.0 nM 5.32
CHEMBL204901 — IC50 = 6700.0 nM 5.17
CHEMBL203864 — IC50 = 7060.0 nM 5.15
CHEMBL205922 — IC50 = 8380.0 nM 5.08
CHEMBL383024 — IC50 = 8380.0 nM 5.08
CHEMBL205024 — IC50 = 9540.0 nM 5.02
CHEMBL204311 — IC50 = 22300.0 nM 4.65
CHEMBL202863 — IC50 = 51000.0 nM 4.29
CHEMBL202684 — IC50 = 64200.0 nM 4.19
CHEMBL203735 — IC50 > 100000.0 nM -
CHEMBL3144705 — IC50 > 100000.0 nM -