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Assay Detail

CHEMBL655786

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

Functional
Tested for cell growth inhibition against CCRF-CEM a human lymphoblastic leukemia line of T-cell origin.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CCRF-CEM
Confidence 1 — Organism
Curated By Expert

Target

CCRF-CEM (CHEMBL382)
Type CELL-LINE
Organism Homo sapiens

Publication

Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition.
Varney MD, Palmer CL, Romines WH, Boritzki T, Margosiak SA, Almassy R, Janson CA, Bartlett C, Howland EJ, Ferre R.
J Med Chem (1997) 40 : 2502 -2524
PubMed 9258357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.12 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84163 1 8.54
CHEMBL82261 1 8.10
CHEMBL85436 1 8.05
CHEMBL82390 1 8.00
CHEMBL309415 1 8.00
CHEMBL315076 1 7.54
CHEMBL85871 1 7.50
CHEMBL84904 1 7.35
CHEMBL84935 1 7.32
CHEMBL315627 1 7.21
CHEMBL84605 1 6.54
CHEMBL84728 1 6.18
CHEMBL85848 1 5.86
CHEMBL82181 1 5.75
CHEMBL84045 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84163 IC50 = 2.9 nM 8.54
CHEMBL82261 IC50 = 8.0 nM 8.10
CHEMBL85436 IC50 = 9.0 nM 8.05
CHEMBL82390 IC50 = 10.0 nM 8.00
CHEMBL309415 IC50 = 10.0 nM 8.00
CHEMBL315076 IC50 = 29.0 nM 7.54
CHEMBL85871 IC50 = 32.0 nM 7.50
CHEMBL84904 IC50 = 45.0 nM 7.35
CHEMBL84935 IC50 = 48.0 nM 7.32
CHEMBL315627 IC50 = 61.0 nM 7.21
CHEMBL84605 IC50 = 290.0 nM 6.54
CHEMBL84728 IC50 = 660.0 nM 6.18
CHEMBL85848 IC50 = 1390.0 nM 5.86
CHEMBL82181 IC50 = 1800.0 nM 5.75
CHEMBL84045 IC50 = 12000.0 nM 4.92