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Assay Detail

CHEMBL5538801

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

Binding
Inhibition of recombinant human DHFR using DHF as substrate measured for 1 hr in presence of NADPH by absorbance based assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigating the anti-cancer potential of pyrimethamine analogues through a modern chemical biology lens.
Brown JI, Persaud R, Iliev P, Karmacharya U, Attarha S, Sahile H, Olsen JE, Hanke D, Idowu T, Frank DA, Frankel A, Williams KC, Page BDG.
Eur J Med Chem (2024) 264 : 115971 -115971
PubMed 38071795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.89 5.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL586281 1 5.26
CHEMBL36 PYRIMETHAMINE 4.0 1 5.17
CHEMBL21414 1 5.09
CHEMBL5575210 1 4.88
CHEMBL5569615 1 4.76
CHEMBL5569327 1 4.65
CHEMBL5565442 1 4.40
CHEMBL5575305 1 -
CHEMBL5569919 1 -
CHEMBL5575876 1 -
CHEMBL5574847 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL586281 IC50 = 5500.0 nM 5.26
CHEMBL36 PYRIMETHAMINE IC50 = 6700.0 nM 5.17
CHEMBL21414 IC50 = 8170.0 nM 5.09
CHEMBL5575210 IC50 = 13200.0 nM 4.88
CHEMBL5569615 IC50 = 17500.0 nM 4.76
CHEMBL5569327 IC50 = 22600.0 nM 4.65
CHEMBL5565442 IC50 = 40000.0 nM 4.40
CHEMBL5575305 IC50 > 100000.0 nM -
CHEMBL5569919 IC50 - -
CHEMBL5575876 IC50 - -
CHEMBL5574847 IC50 > 100000.0 nM -