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Assay Detail

CHEMBL665258

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

Binding
Inhibitory concentration against isolated Pneumocystis carinii DHFR (Dihydrofolate reductase)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Pneumocystis carinii
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Dihydrofolate reductase (CHEMBL1926)
Type SINGLE PROTEIN
Organism Pneumocystis carinii

Publication

Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.
Gangjee A, Yu J, McGuire JJ, Cody V, Galitsky N, Kisliuk RL, Queener SF.
J Med Chem (2000) 43 : 3837 -3851
PubMed 11052789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.20 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.86
CHEMBL439973 1 5.92
CHEMBL1230421 1 4.82
CHEMBL124256 1 -
CHEMBL225072 PEMETREXED 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 13.8 nM 7.86
CHEMBL439973 IC50 = 1200.0 nM 5.92
CHEMBL1230421 IC50 = 15000.0 nM 4.82
CHEMBL124256 IC50 > 19000.0 nM -
CHEMBL225072 PEMETREXED IC50 = 230000.0 nM -