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Assay Detail

CHEMBL655645

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Functional
Growth inhibition of CCRF-CEM human leukemia cells.
7
Total Activities
7
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 Intermediate

Target

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

Publication

Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.
Gangjee A, Zeng Y, McGuire JJ, Kisliuk RL.
J Med Chem (2000) 43 : 3125 -3133
PubMed 10956221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.64 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.84
CHEMBL430872 1 7.54
CHEMBL104829 FURO[2,3D]PYRIMIDINE ANTIFOLATE 1 7.33
CHEMBL106628 1 6.85
CHEMBL323565 1 6.54
CHEMBL1237205 1 5.93
CHEMBL2092925 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE EC50 = 14.4 nM 7.84
CHEMBL430872 EC50 = 29.2 nM 7.54
CHEMBL104829 FURO[2,3D]PYRIMIDINE ANTIFOLATE EC50 = 47.0 nM 7.33
CHEMBL106628 EC50 = 142.0 nM 6.85
CHEMBL323565 EC50 = 290.0 nM 6.54
CHEMBL1237205 EC50 = 1175.0 nM 5.93
CHEMBL2092925 EC50 = 34000.0 nM 4.47