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Assay Detail

CHEMBL4768939

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

ADMET
Inhibition of human DHFR expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis
24
Total Activities
24
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

Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
Kamchonwongpaisan S,Charoensetakul N,Srisuwannaket C,Taweechai S,Rattanajak R,Vanichtanankul J,Vitsupakorn D,Arwon U,Thongpanchang C,Tarnchompoo B,Vilaivan T,Yuthavong Y
Eur J Med Chem (2020) 195 : 112263 -112263
PubMed 32294614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 4.50 4.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129788 1 4.84
CHEMBL4792349 1 4.71
CHEMBL4798400 1 4.68
CHEMBL1231612 1 4.63
CHEMBL4780298 1 4.62
CHEMBL4795771 1 4.62
CHEMBL4789322 1 4.62
CHEMBL4796933 1 4.60
CHEMBL4780381 1 4.54
CHEMBL587606 1 4.54
CHEMBL4793581 1 4.48
CHEMBL4784036 1 4.44
CHEMBL4782529 1 4.42
CHEMBL4796554 1 4.41
CHEMBL4799272 1 4.41
CHEMBL4778245 1 4.38
CHEMBL528489 1 4.37
CHEMBL527468 1 4.34
CHEMBL4784738 1 4.32
CHEMBL4792035 1 4.04
CHEMBL4781149 1 -
CHEMBL4781162 1 -
CHEMBL4800362 1 -
CHEMBL4797103 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129788 Ki = 14600.0 nM 4.84
CHEMBL4792349 Ki = 19500.0 nM 4.71
CHEMBL4798400 Ki = 21100.0 nM 4.68
CHEMBL1231612 Ki = 23600.0 nM 4.63
CHEMBL4780298 Ki = 23700.0 nM 4.62
CHEMBL4795771 Ki = 23700.0 nM 4.62
CHEMBL4789322 Ki = 23700.0 nM 4.62
CHEMBL4796933 Ki = 25200.0 nM 4.60
CHEMBL4780381 Ki = 29200.0 nM 4.54
CHEMBL587606 Ki = 29100.0 nM 4.54
CHEMBL4793581 Ki = 33200.0 nM 4.48
CHEMBL4784036 Ki = 36300.0 nM 4.44
CHEMBL4782529 Ki = 37600.0 nM 4.42
CHEMBL4796554 Ki = 39100.0 nM 4.41
CHEMBL4799272 Ki = 39100.0 nM 4.41
CHEMBL4778245 Ki = 41700.0 nM 4.38
CHEMBL528489 Ki = 42900.0 nM 4.37
CHEMBL527468 Ki = 45800.0 nM 4.34
CHEMBL4784738 Ki = 48400.0 nM 4.32
CHEMBL4792035 Ki = 91500.0 nM 4.04
CHEMBL4781149 Ki = 124000.0 nM -
CHEMBL4781162 Ki = 116000.0 nM -
CHEMBL4800362 Ki = 145000.0 nM -
CHEMBL4797103 Ki = 230000.0 nM -