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Assay Detail

CHEMBL990799

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

Binding
Inhibition of c-kit
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.
Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E.
Bioorg Med Chem Lett (2008) 18 : 5115 -5117
PubMed 18723346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.07 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490823 1 9.00
CHEMBL488984 1 9.00
CHEMBL523816 1 8.70
CHEMBL489196 1 8.52
CHEMBL491429 1 8.52
CHEMBL488985 1 8.40
CHEMBL484885 1 8.40
CHEMBL519520 1 8.30
CHEMBL489579 1 8.15
CHEMBL489786 1 8.15
CHEMBL490407 1 8.10
CHEMBL491628 1 7.96
CHEMBL484883 1 7.96
CHEMBL490408 1 7.96
CHEMBL259247 1 7.85
CHEMBL491238 1 7.70
CHEMBL521788 1 7.55
CHEMBL941 IMATINIB 4.0 1 7.24
CHEMBL484884 1 7.23
CHEMBL491418 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490823 IC50 = 1.0 nM 9.00
CHEMBL488984 IC50 = 1.0 nM 9.00
CHEMBL523816 IC50 = 2.0 nM 8.70
CHEMBL489196 IC50 = 3.0 nM 8.52
CHEMBL491429 IC50 = 3.0 nM 8.52
CHEMBL488985 IC50 = 4.0 nM 8.40
CHEMBL484885 IC50 = 4.0 nM 8.40
CHEMBL519520 IC50 = 5.0 nM 8.30
CHEMBL489579 IC50 = 7.0 nM 8.15
CHEMBL489786 IC50 = 7.0 nM 8.15
CHEMBL490407 IC50 = 8.0 nM 8.10
CHEMBL491628 IC50 = 11.0 nM 7.96
CHEMBL484883 IC50 = 11.0 nM 7.96
CHEMBL490408 IC50 = 11.0 nM 7.96
CHEMBL259247 IC50 = 14.0 nM 7.85
CHEMBL491238 IC50 = 20.0 nM 7.70
CHEMBL521788 IC50 = 28.0 nM 7.55
CHEMBL941 IMATINIB IC50 = 58.0 nM 7.24
CHEMBL484884 IC50 = 59.0 nM 7.23
CHEMBL491418 IC50 = 170.0 nM 6.77