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Assay Detail

CHEMBL5109396

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

Functional
Antiproliferative activity against bortezomib- resistant human KM3/BTZ cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KM3/BTZ
Confidence 1 — Organism
Curated By Autocuration

Target

KM3/BTZ (CHEMBL4483251)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.
Zheng X, Li X, Tian L, Wu B, Yu J, Wang C, Sun X, Ma X, Chen L, Li Y.
Eur J Med Chem (2022) 241 : 114607 -114607
PubMed 35872546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.78 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5176990 1 6.80
CHEMBL5192604 1 6.58
CHEMBL5190968 1 6.30
CHEMBL5186801 1 5.99
CHEMBL5204729 1 5.79
CHEMBL5187385 1 5.67
CHEMBL5196177 1 5.64
CHEMBL5197230 1 5.63
CHEMBL5170906 1 5.60
CHEMBL5177776 1 5.59
CHEMBL5176233 1 5.54
CHEMBL5180558 1 5.43
CHEMBL458997 1 5.36
CHEMBL5177168 1 5.01
CHEMBL5178369 1 -
CHEMBL5195974 1 -
CHEMBL5188293 1 -
CHEMBL5199835 1 -
CHEMBL5206909 1 -
CHEMBL5198068 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5176990 IC50 = 158.6 nM 6.80
CHEMBL5192604 IC50 = 262.3 nM 6.58
CHEMBL5190968 IC50 = 496.6 nM 6.30
CHEMBL5186801 IC50 = 1025.0 nM 5.99
CHEMBL5204729 IC50 = 1613.0 nM 5.79
CHEMBL5187385 IC50 = 2160.0 nM 5.67
CHEMBL5196177 IC50 = 2286.0 nM 5.64
CHEMBL5197230 IC50 = 2315.0 nM 5.63
CHEMBL5170906 IC50 = 2491.0 nM 5.60
CHEMBL5177776 IC50 = 2581.0 nM 5.59
CHEMBL5176233 IC50 = 2886.0 nM 5.54
CHEMBL5180558 IC50 = 3680.0 nM 5.43
CHEMBL458997 IC50 = 4386.0 nM 5.36
CHEMBL5177168 IC50 = 9772.0 nM 5.01
CHEMBL5178369 IC50 > 10000.0 nM -
CHEMBL5195974 IC50 > 10000.0 nM -
CHEMBL5188293 IC50 > 10000.0 nM -
CHEMBL5199835 IC50 > 10000.0 nM -
CHEMBL5206909 IC50 > 10000.0 nM -
CHEMBL5198068 IC50 > 10000.0 nM -