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Assay Detail

CHEMBL4329966

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

ADMET
Inhibition of human DHFR assessed as reduction in NADPH consumption by spectrophotometric method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dihydrofolate reductase (CHEMBL202)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hybrid Inhibitors of Malarial Dihydrofolate Reductase with Dual Binding Modes That Can Forestall Resistance.
Tarnchompoo B, Chitnumsub P, Jaruwat A, Shaw PJ, Vanichtanankul J, Poen S, Rattanajak R, Wongsombat C, Tonsomboon A, Decharuangsilp S, Anukunwithaya T, Arwon U, Kamchonwongpaisan S, Yuthavong Y.
ACS Med Chem Lett (2018) 9 : 1235 -1240
PubMed 30613332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.58 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4462726 1 7.74
CHEMBL4454693 1 7.70
CHEMBL4442735 1 7.65
CHEMBL4460601 1 7.47
CHEMBL3819601 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4462726 Ki = 18.1 nM 7.74
CHEMBL4454693 Ki = 20.2 nM 7.70
CHEMBL4442735 Ki = 22.5 nM 7.65
CHEMBL4460601 Ki = 33.6 nM 7.47
CHEMBL3819601 Ki = 47.6 nM 7.32