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Assay Detail

CHEMBL677017

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

Functional
Inhibition of cellular growth against human adenocarcinoma (GC3/M TK-) deficient in thymidine kinase.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type GC3/MTK-
Confidence 1 — Organism
Curated By Intermediate

Target

GC3/MTK- (CHEMBL614157)
Type CELL-LINE
Organism Homo sapiens

Publication

Design of enzyme inhibitors using iterative protein crystallographic analysis.
Appelt K, Bacquet RJ, Bartlett CA, Booth CL, Freer ST, Fuhry MA, Gehring MR, Herrmann SM, Howland EF, Janson CA.
J Med Chem (1991) 34 : 1925 -1934
PubMed 2066965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.46 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25889 1 7.31
CHEMBL417222 1 5.96
CHEMBL422395 1 5.85
CHEMBL299928 1 5.82
CHEMBL275685 1 5.34
CHEMBL291548 1 5.12
CHEMBL56992 1 4.80
CHEMBL57002 1 4.60
CHEMBL353700 1 4.37
CHEMBL57333 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25889 IC50 = 49.0 nM 7.31
CHEMBL417222 IC50 = 1100.0 nM 5.96
CHEMBL422395 IC50 = 1400.0 nM 5.85
CHEMBL299928 IC50 = 1500.0 nM 5.82
CHEMBL275685 IC50 = 4600.0 nM 5.34
CHEMBL291548 IC50 = 7500.0 nM 5.12
CHEMBL56992 IC50 = 16000.0 nM 4.80
CHEMBL57002 IC50 = 25000.0 nM 4.60
CHEMBL353700 IC50 = 43000.0 nM 4.37
CHEMBL57333 IC50 > 10700.0 nM -