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Assay Detail

CHEMBL667223

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Binding
Inhibitory activity against dihydrofolate reductase in rat liver
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL2363)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 10. 2,4-Diamino-5-(6-quinolylmethyl)- and -[(tetrahydro-6-quinolyl)methyl]pyrimidine derivatives. Further specificity studies.
Rauckman BS, Tidwell MY, Johnson JV, Roth B.
J Med Chem (1989) 32 : 1927 -1935
PubMed 2502632 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 4.54 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58455 1 5.24
CHEMBL57900 1 5.00
CHEMBL293325 1 4.92
CHEMBL441616 1 4.82
CHEMBL57459 1 4.75
CHEMBL294638 1 4.70
CHEMBL60632 1 4.66
CHEMBL59283 1 4.66
CHEMBL58744 1 4.50
CHEMBL58038 1 4.48
CHEMBL56652 1 4.42
CHEMBL60636 1 4.39
CHEMBL57377 1 4.37
CHEMBL57812 1 4.36
CHEMBL57458 1 4.36
CHEMBL57807 1 4.21
CHEMBL293977 1 4.19
CHEMBL301628 1 4.12
CHEMBL60582 1 4.05
CHEMBL59491 1 -
CHEMBL58074 1 -
CHEMBL292839 1 -
CHEMBL292621 1 -
CHEMBL61260 1 -
CHEMBL58917 1 -
CHEMBL57829 1 -
CHEMBL58075 1 -
CHEMBL22 TRIMETHOPRIM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58455 IC50 = 5700.0 nM 5.24
CHEMBL57900 IC50 = 9900.0 nM 5.00
CHEMBL293325 IC50 = 12000.0 nM 4.92
CHEMBL441616 IC50 = 15000.0 nM 4.82
CHEMBL57459 IC50 = 18000.0 nM 4.75
CHEMBL294638 IC50 = 20000.0 nM 4.70
CHEMBL60632 IC50 = 22000.0 nM 4.66
CHEMBL59283 IC50 = 22000.0 nM 4.66
CHEMBL58744 IC50 = 32000.0 nM 4.50
CHEMBL58038 IC50 = 33000.0 nM 4.48
CHEMBL56652 IC50 = 38000.0 nM 4.42
CHEMBL60636 IC50 = 41000.0 nM 4.39
CHEMBL57377 IC50 = 43000.0 nM 4.37
CHEMBL57812 IC50 = 44000.0 nM 4.36
CHEMBL57458 IC50 = 44000.0 nM 4.36
CHEMBL57807 IC50 = 61000.0 nM 4.21
CHEMBL293977 IC50 = 64000.0 nM 4.19
CHEMBL301628 IC50 = 76000.0 nM 4.12
CHEMBL60582 IC50 = 89000.0 nM 4.05
CHEMBL59491 IC50 = 250000.0 nM -
CHEMBL58074 IC50 = 142000.0 nM -
CHEMBL292839 IC50 = 190000.0 nM -
CHEMBL292621 IC50 = 142000.0 nM -
CHEMBL61260 IC50 = 170000.0 nM -
CHEMBL58917 IC50 = 140000.0 nM -
CHEMBL57829 IC50 = 440000.0 nM -
CHEMBL58075 IC50 = 260000.0 nM -
CHEMBL22 TRIMETHOPRIM IC50 = 340000.0 nM -