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Assay Detail

CHEMBL4828519

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

Functional
Growth inhibition of human KARPAS-422 cells assessed as cell growth incubated for 7 days by lactate dehydrogenase based WST-8 assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KARPAS-422
Confidence 1 — Organism
Curated By Autocuration

Target

KARPAS-422 (CHEMBL2366368)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.
Rej RK, Wang C, Lu J, Wang M, Petrunak E, Zawacki KP, McEachern D, Yang CY, Wang L, Li R, Chinnaswamy K, Wen B, Sun D, Stuckey JA, Zhou Y, Chen J, Tang G, Wang S.
J Med Chem (2021) 64 : 14540 -14556
PubMed 34613724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 8.31 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4859559 1 9.30
CHEMBL4869420 1 9.05
CHEMBL4850823 1 9.00
CHEMBL4877375 1 9.00
CHEMBL4861394 1 8.92
CHEMBL4854800 1 8.92
CHEMBL4870920 1 8.92
CHEMBL4871261 1 8.89
CHEMBL4861749 1 8.85
CHEMBL4855616 1 8.85
CHEMBL4850847 1 8.82
CHEMBL4873268 1 8.72
CHEMBL4857414 1 8.72
CHEMBL4856280 1 8.70
CHEMBL4878932 1 8.66
CHEMBL4858089 1 8.62
CHEMBL4860499 1 8.51
CHEMBL4856160 1 8.41
CHEMBL4851576 1 8.38
CHEMBL4847943 1 8.36
CHEMBL4849266 1 8.34
CHEMBL4858561 1 8.20
CHEMBL4877695 1 8.18
CHEMBL4872891 1 8.10
CHEMBL4865691 1 8.09
CHEMBL4862163 1 8.08
CHEMBL4854206 1 7.83
CHEMBL4847397 1 7.76
CHEMBL4869720 1 7.54
CHEMBL4869748 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4859559 IC50 = 0.5 nM 9.30
CHEMBL4869420 IC50 = 0.9 nM 9.05
CHEMBL4850823 IC50 = 1.0 nM 9.00
CHEMBL4877375 IC50 = 1.0 nM 9.00
CHEMBL4861394 IC50 = 1.2 nM 8.92
CHEMBL4854800 IC50 = 1.2 nM 8.92
CHEMBL4870920 IC50 = 1.2 nM 8.92
CHEMBL4871261 IC50 = 1.3 nM 8.89
CHEMBL4861749 IC50 = 1.4 nM 8.85
CHEMBL4855616 IC50 = 1.4 nM 8.85
CHEMBL4850847 IC50 = 1.5 nM 8.82
CHEMBL4873268 IC50 = 1.9 nM 8.72
CHEMBL4857414 IC50 = 1.9 nM 8.72
CHEMBL4856280 IC50 = 2.0 nM 8.70
CHEMBL4878932 IC50 = 2.2 nM 8.66
CHEMBL4858089 IC50 = 2.4 nM 8.62
CHEMBL4860499 IC50 = 3.1 nM 8.51
CHEMBL4856160 IC50 = 3.9 nM 8.41
CHEMBL4851576 IC50 = 4.2 nM 8.38
CHEMBL4847943 IC50 = 4.4 nM 8.36
CHEMBL4849266 IC50 = 4.6 nM 8.34
CHEMBL4858561 IC50 = 6.3 nM 8.20
CHEMBL4877695 IC50 = 6.6 nM 8.18
CHEMBL4872891 IC50 = 7.9 nM 8.10
CHEMBL4865691 IC50 = 8.1 nM 8.09
CHEMBL4862163 IC50 = 8.3 nM 8.08
CHEMBL4854206 IC50 = 14.9 nM 7.83
CHEMBL4847397 IC50 = 17.4 nM 7.76
CHEMBL4869720 IC50 = 29.2 nM 7.54
CHEMBL4869748 IC50 = 37.1 nM 7.43
CHEMBL4869208 IC50 = 51.5 nM 7.29
CHEMBL4858622 IC50 = 57.8 nM 7.24
CHEMBL4104741 IC50 = 62.9 nM 7.20
CHEMBL4861770 IC50 = 68.3 nM 7.17
CHEMBL4065484 IC50 = 125.4 nM 6.90