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Assay Detail

CHEMBL668085

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Binding
Tested for inhibitory activity against dihydrofolate reductase in human
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.
Rosowsky A, Mota CE, Wright JE, Freisheim JH, Heusner JJ, McCormack JJ, Queener SF.
J Med Chem (1993) 36 : 3103 -3112
PubMed 8230096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.04 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119 TRIMETREXATE 4.0 1 8.85
CHEMBL104787 1 6.14
CHEMBL323960 1 6.12
CHEMBL326200 1 -
CHEMBL322585 1 -
CHEMBL322315 1 -
CHEMBL322861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119 TRIMETREXATE IC50 = 1.4 nM 8.85
CHEMBL104787 IC50 = 730.0 nM 6.14
CHEMBL323960 IC50 = 750.0 nM 6.12
CHEMBL326200 IC50 > 10000.0 nM -
CHEMBL322585 IC50 > 10000.0 nM -
CHEMBL322315 IC50 > 10000.0 nM -
CHEMBL322861 IC50 > 10000.0 nM -