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Assay Detail

CHEMBL875148

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Binding
In vitro inhibitory activity against L1210 dihydrofolate reductase in rodent neoplastic cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type L1210
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Dihydrofolate reductase (CHEMBL4564)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

10-Propargylaminopterin and alkyl homologues of methotrexate as inhibitors of folate metabolism.
Piper JR, McCaleb GS, Montgomery JA, Kisliuk RL, Gaumont Y, Sirotnak FM.
J Med Chem (1982) 25 : 877 -880
PubMed 7108907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.53 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166915 1 9.30
CHEMBL171757 1 7.76
CHEMBL376180 AMINOPTERIN 2.0 1 -
CHEMBL34259 METHOTREXATE 4.0 1 -
CHEMBL354055 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166915 Ki = 0.5 nM 9.30
CHEMBL171757 Ki = 17.5 nM 7.76
CHEMBL376180 AMINOPTERIN Ki = 0.004 nM -
CHEMBL34259 METHOTREXATE Ki = 0.006 nM -
CHEMBL354055 Ki = 0.003 nM -