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Assay Detail

CHEMBL731497

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Binding
Inhibitory activity against Mitogen-activated protein kinase p38 alpha 2
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.
Dumas J, Hatoum-Mokdad H, Sibley RN, Smith RA, Scott WJ, Khire U, Lee W, Wood J, Wolanin D, Cooley J, Bankston D, Redman AM, Schoenleber R, Caringal Y, Gunn D, Romero R, Osterhout M, Paulsen H, Housley TJ, Wilhelm SM, Pirro J, Chien DS, Ranges GE, Shrikhande A, Muzsi A, Bortolon E, Wakefield J, Gianpaolo Ostravage C, Bhargava A, Chau T.
Bioorg Med Chem Lett (2002) 12 : 1559 -1562
PubMed 12039561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.05 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41723 1 7.89
CHEMBL10 SB-203580 1 7.70
CHEMBL41310 1 7.48
CHEMBL290971 1 7.46
CHEMBL415679 1 7.43
CHEMBL290982 1 7.42
CHEMBL288812 1 7.38
CHEMBL40138 1 7.36
CHEMBL40166 1 7.35
CHEMBL41653 1 7.28
CHEMBL288663 1 7.27
CHEMBL288891 1 7.24
CHEMBL38548 1 7.16
CHEMBL288889 1 7.16
CHEMBL416425 1 7.16
CHEMBL38625 1 7.06
CHEMBL38084 1 6.96
CHEMBL37353 1 6.85
CHEMBL39251 1 6.80
CHEMBL289056 1 6.74
CHEMBL40020 1 6.70
CHEMBL289155 1 6.63
CHEMBL39136 1 6.58
CHEMBL41970 1 6.57
CHEMBL39931 1 6.54
CHEMBL41266 1 6.51
CHEMBL289357 1 6.38
CHEMBL38648 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41723 IC50 = 13.0 nM 7.89
CHEMBL10 SB-203580 IC50 = 20.0 nM 7.70
CHEMBL41310 IC50 = 33.0 nM 7.48
CHEMBL290971 IC50 = 35.0 nM 7.46
CHEMBL415679 IC50 = 37.0 nM 7.43
CHEMBL290982 IC50 = 38.0 nM 7.42
CHEMBL288812 IC50 = 42.0 nM 7.38
CHEMBL40138 IC50 = 44.0 nM 7.36
CHEMBL40166 IC50 = 45.0 nM 7.35
CHEMBL41653 IC50 = 53.0 nM 7.28
CHEMBL288663 IC50 = 54.0 nM 7.27
CHEMBL288891 IC50 = 57.0 nM 7.24
CHEMBL38548 IC50 = 69.0 nM 7.16
CHEMBL288889 IC50 = 69.0 nM 7.16
CHEMBL416425 IC50 = 70.0 nM 7.16
CHEMBL38625 IC50 = 87.0 nM 7.06
CHEMBL38084 IC50 = 110.0 nM 6.96
CHEMBL37353 IC50 = 140.0 nM 6.85
CHEMBL39251 IC50 = 160.0 nM 6.80
CHEMBL289056 IC50 = 183.0 nM 6.74
CHEMBL40020 IC50 = 200.0 nM 6.70
CHEMBL289155 IC50 = 235.0 nM 6.63
CHEMBL39136 IC50 = 260.0 nM 6.58
CHEMBL41970 IC50 = 270.0 nM 6.57
CHEMBL39931 IC50 = 290.0 nM 6.54
CHEMBL41266 IC50 = 310.0 nM 6.51
CHEMBL289357 IC50 = 420.0 nM 6.38
CHEMBL38648 IC50 = 430.0 nM 6.37