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Assay Detail

CHEMBL732963

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Binding
Inhibitory activity against Mitogen-activated protein kinase p38 alpha 2 expressed in Escherichia coli.
19
Total Activities
19
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

Discovery of a new class of p38 kinase inhibitors.
Dumas J, Sibley R, Riedl B, Monahan MK, Lee W, Lowinger TB, Redman AM, Johnson JS, Kingery-Wood J, Scott WJ, Smith RA, Bobko M, Schoenleber R, Ranges GE, Housley TJ, Bhargava A, Wilhelm SM, Shrikhande A.
Bioorg Med Chem Lett (2000) 10 : 2047 -2050
PubMed 10999467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62794 1 8.70
CHEMBL10 SB-203580 1 7.70
CHEMBL292482 1 7.44
CHEMBL41653 1 7.28
CHEMBL302379 1 7.24
CHEMBL62788 1 7.00
CHEMBL64510 1 6.92
CHEMBL304936 1 6.92
CHEMBL62008 1 6.92
CHEMBL64075 1 6.80
CHEMBL59652 1 6.72
CHEMBL62946 1 6.70
CHEMBL65671 1 6.66
CHEMBL61510 1 6.58
CHEMBL61628 1 6.54
CHEMBL291413 1 6.43
CHEMBL62665 1 6.15
CHEMBL64644 1 6.04
CHEMBL63101 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62794 IC50 = 2.0 nM 8.70
CHEMBL10 SB-203580 IC50 = 20.0 nM 7.70
CHEMBL292482 IC50 = 36.0 nM 7.44
CHEMBL41653 IC50 = 53.0 nM 7.28
CHEMBL302379 IC50 = 58.0 nM 7.24
CHEMBL62788 IC50 = 100.0 nM 7.00
CHEMBL64510 IC50 = 120.0 nM 6.92
CHEMBL304936 IC50 = 120.0 nM 6.92
CHEMBL62008 IC50 = 120.0 nM 6.92
CHEMBL64075 IC50 = 160.0 nM 6.80
CHEMBL59652 IC50 = 190.0 nM 6.72
CHEMBL62946 IC50 = 200.0 nM 6.70
CHEMBL65671 IC50 = 220.0 nM 6.66
CHEMBL61510 IC50 = 260.0 nM 6.58
CHEMBL61628 IC50 = 290.0 nM 6.54
CHEMBL291413 IC50 = 370.0 nM 6.43
CHEMBL62665 IC50 = 710.0 nM 6.15
CHEMBL64644 IC50 = 920.0 nM 6.04
CHEMBL63101 IC50 = 1100.0 nM 5.96