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Assay Detail

CHEMBL867362

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Binding
Inhibition of p38alpha
28
Total Activities
28
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

p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones.
Natarajan SR, Wisnoski DD, Thompson JE, O'Neill EA, O'Keefe SJ.
Bioorg Med Chem Lett (2006) 16 : 4400 -4404
PubMed 16750629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.74 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212549 1 9.70
CHEMBL319556 1 9.70
CHEMBL212803 1 9.30
CHEMBL211795 1 9.30
CHEMBL377979 1 9.22
CHEMBL209442 1 9.15
CHEMBL214138 1 9.10
CHEMBL96632 1 9.00
CHEMBL213142 1 9.00
CHEMBL213895 1 8.96
CHEMBL212091 1 8.92
CHEMBL213986 1 8.72
CHEMBL94556 1 8.70
CHEMBL211303 1 8.70
CHEMBL378717 1 8.70
CHEMBL210110 1 8.70
CHEMBL213836 1 8.70
CHEMBL425785 1 8.70
CHEMBL441853 1 8.52
CHEMBL213846 1 8.40
CHEMBL215651 1 8.40
CHEMBL211426 1 8.38
CHEMBL212937 1 8.38
CHEMBL212821 1 8.28
CHEMBL213190 1 8.25
CHEMBL425422 1 8.22
CHEMBL212753 1 8.00
CHEMBL425265 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212549 IC50 = 0.2 nM 9.70
CHEMBL319556 IC50 = 0.2 nM 9.70
CHEMBL212803 IC50 = 0.5 nM 9.30
CHEMBL211795 IC50 = 0.5 nM 9.30
CHEMBL377979 IC50 = 0.6 nM 9.22
CHEMBL209442 IC50 = 0.7 nM 9.15
CHEMBL214138 IC50 = 0.8 nM 9.10
CHEMBL96632 IC50 = 1.0 nM 9.00
CHEMBL213142 IC50 = 1.0 nM 9.00
CHEMBL213895 IC50 = 1.1 nM 8.96
CHEMBL212091 IC50 = 1.2 nM 8.92
CHEMBL213986 IC50 = 1.9 nM 8.72
CHEMBL94556 IC50 = 2.0 nM 8.70
CHEMBL211303 IC50 = 2.0 nM 8.70
CHEMBL378717 IC50 = 2.0 nM 8.70
CHEMBL210110 IC50 = 2.0 nM 8.70
CHEMBL213836 IC50 = 2.0 nM 8.70
CHEMBL425785 IC50 = 2.0 nM 8.70
CHEMBL441853 IC50 = 3.0 nM 8.52
CHEMBL213846 IC50 = 4.0 nM 8.40
CHEMBL215651 IC50 = 4.0 nM 8.40
CHEMBL211426 IC50 = 4.2 nM 8.38
CHEMBL212937 IC50 = 4.2 nM 8.38
CHEMBL212821 IC50 = 5.3 nM 8.28
CHEMBL213190 IC50 = 5.6 nM 8.25
CHEMBL425422 IC50 = 6.0 nM 8.22
CHEMBL212753 IC50 = 10.0 nM 8.00
CHEMBL425265 IC50 = 20.0 nM 7.70