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Assay Detail

CHEMBL5047786

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

Binding
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate in presence of ATP incubated for 60 mins by ADP-glo based luminescence assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.
Wu CF, Wang QC, Chen R, Zhou HL, Wu TT, Du Y, Zhang NN, Zhang HM, Fan ZY, Wang LL, Hu CJ, Sang ZP, Li HL, Wang L, Tang L, Zhang JQ.
Eur J Med Chem (2022) 229 : 114055 -114055
PubMed 34971874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.26 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5074018 1 9.22
CHEMBL5091789 1 9.22
CHEMBL5071942 1 9.15
CHEMBL5076528 1 9.15
CHEMBL5093540 1 9.05
CHEMBL5091543 1 8.80
CHEMBL5079887 1 8.80
CHEMBL5080996 1 8.74
CHEMBL5083002 1 8.72
CHEMBL5078347 1 8.37
CHEMBL5085872 1 8.37
CHEMBL5071085 1 8.30
CHEMBL5084675 1 8.26
CHEMBL5083425 1 8.24
CHEMBL592445 GEDATOLISIB 3.0 1 8.22
CHEMBL5079231 1 8.15
CHEMBL5071429 1 8.04
CHEMBL5079397 1 7.99
CHEMBL5094579 1 7.96
CHEMBL5085515 1 7.86
CHEMBL5086413 1 7.78
CHEMBL5086369 1 7.72
CHEMBL5089561 1 7.54
CHEMBL5073129 1 7.54
CHEMBL5070586 1 7.50
CHEMBL5074924 1 6.17
CHEMBL5087707 1 -
CHEMBL5089743 1 -
CHEMBL5087372 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5074018 IC50 = 0.6 nM 9.22
CHEMBL5091789 IC50 = 0.6 nM 9.22
CHEMBL5071942 IC50 = 0.7 nM 9.15
CHEMBL5076528 IC50 = 0.7 nM 9.15
CHEMBL5093540 IC50 = 0.9 nM 9.05
CHEMBL5091543 IC50 = 1.6 nM 8.80
CHEMBL5079887 IC50 = 1.6 nM 8.80
CHEMBL5080996 IC50 = 1.8 nM 8.74
CHEMBL5083002 IC50 = 1.9 nM 8.72
CHEMBL5078347 IC50 = 4.3 nM 8.37
CHEMBL5085872 IC50 = 4.3 nM 8.37
CHEMBL5071085 IC50 = 5.0 nM 8.30
CHEMBL5084675 IC50 = 5.5 nM 8.26
CHEMBL5083425 IC50 = 5.7 nM 8.24
CHEMBL592445 GEDATOLISIB IC50 = 6.0 nM 8.22
CHEMBL5079231 IC50 = 7.0 nM 8.15
CHEMBL5071429 IC50 = 9.1 nM 8.04
CHEMBL5079397 IC50 = 10.2 nM 7.99
CHEMBL5094579 IC50 = 11.0 nM 7.96
CHEMBL5085515 IC50 = 13.8 nM 7.86
CHEMBL5086413 IC50 = 16.5 nM 7.78
CHEMBL5086369 IC50 = 19.0 nM 7.72
CHEMBL5089561 IC50 = 28.7 nM 7.54
CHEMBL5073129 IC50 = 28.7 nM 7.54
CHEMBL5070586 IC50 = 31.8 nM 7.50
CHEMBL5074924 IC50 = 680.0 nM 6.17
CHEMBL5087707 IC50 > 1000.0 nM -
CHEMBL5089743 IC50 > 1000.0 nM -
CHEMBL5087372 IC50 > 1000.0 nM -