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Assay Detail

CHEMBL955809

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of p38 by TR-FRET assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.
Hu E, Tasker A, White RD, Kunz RK, Human J, Chen N, Bürli R, Hungate R, Novak P, Itano A, Zhang X, Yu V, Nguyen Y, Tudor Y, Plant M, Flynn S, Xu Y, Meagher KL, Whittington DA, Ng GY.
J Med Chem (2008) 51 : 3065 -3068
PubMed 18447379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.32 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496494 1 7.55
CHEMBL493986 1 6.70
CHEMBL487431 1 6.00
CHEMBL497343 1 5.42
CHEMBL498557 1 5.41
CHEMBL497958 1 5.35
CHEMBL522905 1 5.31
CHEMBL494821 1 5.24
CHEMBL504805 1 5.21
CHEMBL506033 1 5.19
CHEMBL496713 1 5.12
CHEMBL496916 1 5.10
CHEMBL497754 1 5.04
CHEMBL941 IMATINIB 4.0 1 4.85
CHEMBL496505 1 4.75
CHEMBL525744 1 4.68
CHEMBL497957 1 4.40
CHEMBL525893 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496494 IC50 = 28.0 nM 7.55
CHEMBL493986 IC50 = 200.0 nM 6.70
CHEMBL487431 IC50 = 990.0 nM 6.00
CHEMBL497343 IC50 = 3800.0 nM 5.42
CHEMBL498557 IC50 = 3900.0 nM 5.41
CHEMBL497958 IC50 = 4500.0 nM 5.35
CHEMBL522905 IC50 = 4900.0 nM 5.31
CHEMBL494821 IC50 = 5800.0 nM 5.24
CHEMBL504805 IC50 = 6100.0 nM 5.21
CHEMBL506033 IC50 = 6500.0 nM 5.19
CHEMBL496713 IC50 = 7500.0 nM 5.12
CHEMBL496916 IC50 = 8000.0 nM 5.10
CHEMBL497754 IC50 = 9200.0 nM 5.04
CHEMBL941 IMATINIB IC50 = 14000.0 nM 4.85
CHEMBL496505 IC50 = 18000.0 nM 4.75
CHEMBL525744 IC50 = 21000.0 nM 4.68
CHEMBL497957 IC50 = 40000.0 nM 4.40
CHEMBL525893 IC50 = 40000.0 nM 4.40