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Assay Detail

CHEMBL659476

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

Functional
Tested for inhibition of [14C]-DDATHF influx in CEM/MTX cells of human leukemic lymphoblasts
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CCRF-CEM
Confidence 1 — Organism
Curated By Intermediate

Target

CCRF-CEM (CHEMBL382)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological activity of N omega-hemiphthaloyl-alpha,omega- diaminoalkanoic acid analogues of aminopterin and 3',5-dichloroaminopterin.
Rosowsky A, Bader H, Wright JE, Keyomarsi K, Matherly LH.
J Med Chem (1994) 37 : 2167 -2174
PubMed 8035423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.64 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18155 1 6.36
CHEMBL1679 LEUCOVORIN 4.0 1 6.13
CHEMBL1622 FOLIC ACID 4.0 1 5.05
CHEMBL34259 METHOTREXATE 4.0 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18155 Ki = 440.0 nM 6.36
CHEMBL1679 LEUCOVORIN Ki = 740.0 nM 6.13
CHEMBL1622 FOLIC ACID Ki = 8950.0 nM 5.05
CHEMBL34259 METHOTREXATE Ki = 9740.0 nM 5.01