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Assay Detail

CHEMBL668876

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

Binding
In vitro inhibitory concentration against rat liver dihydrofolate reductase(DHFR)
18
Total Activities
18
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

Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cell line.
Griffin RJ, Meek MA, Schwalbe CH, Stevens MF.
J Med Chem (1989) 32 : 2468 -2474
PubMed 2810335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.76 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312667 1 7.70
CHEMBL59530 1 7.10
CHEMBL79407 1 7.00
CHEMBL81552 1 6.36
CHEMBL82208 1 5.77
CHEMBL79279 1 5.51
CHEMBL79465 1 5.41
CHEMBL263275 1 5.40
CHEMBL309217 1 5.21
CHEMBL80110 1 5.10
CHEMBL80067 1 5.07
CHEMBL82464 1 5.04
CHEMBL314593 1 4.17
CHEMBL83283 1 -
CHEMBL311176 1 -
CHEMBL439949 1 -
CHEMBL79883 1 -
CHEMBL79417 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312667 IC50 = 20.0 nM 7.70
CHEMBL59530 IC50 = 80.0 nM 7.10
CHEMBL79407 IC50 = 100.0 nM 7.00
CHEMBL81552 IC50 = 440.0 nM 6.36
CHEMBL82208 IC50 = 1700.0 nM 5.77
CHEMBL79279 IC50 = 3100.0 nM 5.51
CHEMBL79465 IC50 = 3900.0 nM 5.41
CHEMBL263275 IC50 = 4000.0 nM 5.40
CHEMBL309217 IC50 = 6200.0 nM 5.21
CHEMBL80110 IC50 = 8000.0 nM 5.10
CHEMBL80067 IC50 = 8500.0 nM 5.07
CHEMBL82464 IC50 = 9200.0 nM 5.04
CHEMBL314593 IC50 = 67000.0 nM 4.17
CHEMBL83283 IC50 > 25000.0 nM -
CHEMBL311176 IC50 > 25000.0 nM -
CHEMBL439949 IC50 > 25000.0 nM -
CHEMBL79883 IC50 > 25000.0 nM -
CHEMBL79417 IC50 > 25000.0 nM -