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Assay Detail

CHEMBL1243604

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Binding
Inhibition of cKIT
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.
Cao H, Zhang H, Zheng X, Gao D.
J Mol Graph Model (2007) 26 : 236 -245
PubMed 17293140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.11 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196363 1 8.22
CHEMBL371329 1 8.05
CHEMBL365784 1 7.82
CHEMBL371889 1 7.72
CHEMBL371206 1 7.72
CHEMBL382517 1 7.66
CHEMBL198297 1 7.59
CHEMBL196747 1 7.57
CHEMBL425749 1 7.57
CHEMBL366241 1 7.55
CHEMBL370545 1 7.55
CHEMBL372174 1 7.54
CHEMBL197592 1 7.49
CHEMBL196499 1 7.48
CHEMBL197353 1 7.43
CHEMBL371510 1 7.42
CHEMBL1242107 1 7.37
CHEMBL194236 1 7.32
CHEMBL195955 1 7.30
CHEMBL445394 1 7.30
CHEMBL196615 1 7.27
CHEMBL438797 1 7.17
CHEMBL371225 1 7.09
CHEMBL198267 1 7.08
CHEMBL194321 1 6.96
CHEMBL370325 1 6.85
CHEMBL197635 1 6.80
CHEMBL381034 1 6.76
CHEMBL194366 1 6.74
CHEMBL381207 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196363 IC50 = 6.026 nM 8.22
CHEMBL371329 IC50 = 8.913 nM 8.05
CHEMBL365784 IC50 = 15.14 nM 7.82
CHEMBL371889 IC50 = 19.05 nM 7.72
CHEMBL371206 IC50 = 19.05 nM 7.72
CHEMBL382517 IC50 = 21.88 nM 7.66
CHEMBL198297 IC50 = 25.7 nM 7.59
CHEMBL196747 IC50 = 26.92 nM 7.57
CHEMBL425749 IC50 = 26.92 nM 7.57
CHEMBL370545 IC50 = 28.18 nM 7.55
CHEMBL366241 IC50 = 28.18 nM 7.55
CHEMBL372174 IC50 = 28.84 nM 7.54
CHEMBL197592 IC50 = 32.36 nM 7.49
CHEMBL196499 IC50 = 33.11 nM 7.48
CHEMBL197353 IC50 = 37.15 nM 7.43
CHEMBL371510 IC50 = 38.02 nM 7.42
CHEMBL1242107 IC50 = 42.66 nM 7.37
CHEMBL194236 IC50 = 47.86 nM 7.32
CHEMBL445394 IC50 = 50.12 nM 7.30
CHEMBL195955 IC50 = 50.12 nM 7.30
CHEMBL196615 IC50 = 53.7 nM 7.27
CHEMBL438797 IC50 = 67.61 nM 7.17
CHEMBL371225 IC50 = 81.28 nM 7.09
CHEMBL198267 IC50 = 83.18 nM 7.08
CHEMBL194321 IC50 = 109.65 nM 6.96
CHEMBL370325 IC50 = 141.25 nM 6.85
CHEMBL197635 IC50 = 158.49 nM 6.80
CHEMBL381034 IC50 = 173.78 nM 6.76
CHEMBL381207 IC50 = 181.97 nM 6.74
CHEMBL194366 IC50 = 181.97 nM 6.74
CHEMBL371332 IC50 = 199.53 nM 6.70
CHEMBL198155 IC50 = 363.08 nM 6.44
CHEMBL198601 IC50 = 398.11 nM 6.40
CHEMBL194842 IC50 = 575.44 nM 6.24
CHEMBL371379 IC50 = 794.33 nM 6.10
CHEMBL372388 IC50 = 794.33 nM 6.10
CHEMBL196636 IC50 = 812.83 nM 6.09
CHEMBL382112 IC50 = 933.25 nM 6.03
CHEMBL369908 IC50 = 954.99 nM 6.02