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Assay Detail

CHEMBL4021200

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

Functional
Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay
28
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1993
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1993 (CHEMBL1075527)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization.
Zhao F, Zhang LD, Hao Y, Chen N, Bai R, Wang YJ, Zhang CC, Li GS, Hao LJ, Shi C, Zhang J, Mao Y, Fan Y, Xia GX, Yu JX, Liu YJ.
Eur J Med Chem (2017) 134 : 147 -158
PubMed 28411455 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.92 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4064183 1 9.70
CHEMBL4076438 1 9.70
CHEMBL4104884 1 9.40
CHEMBL4091023 1 9.30
CHEMBL4074262 3 9.22
CHEMBL4070258 1 9.10
CHEMBL4097173 1 9.10
CHEMBL4060354 1 9.05
CHEMBL4070051 1 9.05
CHEMBL4061378 1 9.05
CHEMBL4083235 1 9.05
CHEMBL4092293 1 8.96
CHEMBL4093803 1 8.92
CHEMBL3188267 CAPMATINIB 4.0 1 8.64
CHEMBL4102466 1 8.59
CHEMBL4068290 1 8.49
CHEMBL4065641 1 8.46
CHEMBL4078192 1 8.44
CHEMBL4094716 1 8.39
CHEMBL4099662 1 8.38
CHEMBL4072776 1 8.06
CHEMBL4073110 1 -
CHEMBL4075149 1 -
CHEMBL4081567 1 -
CHEMBL4059611 1 -
CHEMBL4089433 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4064183 IC50 = 0.2 nM 9.70
CHEMBL4076438 IC50 = 0.2 nM 9.70
CHEMBL4104884 IC50 = 0.4 nM 9.40
CHEMBL4091023 IC50 = 0.5 nM 9.30
CHEMBL4074262 IC50 = 0.6 nM 9.22
CHEMBL4074262 IC50 = 0.7 nM 9.15
CHEMBL4070258 IC50 = 0.8 nM 9.10
CHEMBL4097173 IC50 = 0.8 nM 9.10
CHEMBL4083235 IC50 = 0.9 nM 9.05
CHEMBL4060354 IC50 = 0.9 nM 9.05
CHEMBL4061378 IC50 = 0.9 nM 9.05
CHEMBL4070051 IC50 = 0.9 nM 9.05
CHEMBL4074262 IC50 = 1.1 nM 8.96
CHEMBL4092293 IC50 = 1.1 nM 8.96
CHEMBL4093803 IC50 = 1.2 nM 8.92
CHEMBL3188267 CAPMATINIB IC50 = 2.3 nM 8.64
CHEMBL4102466 IC50 = 2.6 nM 8.59
CHEMBL4068290 IC50 = 3.2 nM 8.49
CHEMBL4065641 IC50 = 3.5 nM 8.46
CHEMBL4078192 IC50 = 3.6 nM 8.44
CHEMBL4094716 IC50 = 4.1 nM 8.39
CHEMBL4099662 IC50 = 4.2 nM 8.38
CHEMBL4072776 IC50 = 8.7 nM 8.06
CHEMBL4073110 IC50 - -
CHEMBL4081567 IC50 - -
CHEMBL4059611 IC50 - -
CHEMBL4075149 IC50 - -
CHEMBL4089433 IC50 - -