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Assay Detail

CHEMBL4768935

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Binding
Inhibition of Plasmodium falciparum DHFR C59R/S108T mutant expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

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 49 8.79 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4780298 — — 1 9.30
CHEMBL129788 — — 1 9.22
CHEMBL4792349 — — 1 9.22
CHEMBL4781162 — — 1 9.15
CHEMBL4792035 — — 1 9.15
CHEMBL4778245 — — 1 9.15
CHEMBL4783968 — — 1 9.10
CHEMBL4784738 — — 1 9.10
CHEMBL4793034 — — 1 9.10
CHEMBL587606 — — 1 9.10
CHEMBL4795771 — — 1 9.10
CHEMBL4796933 — — 1 9.10
CHEMBL4782529 — — 1 9.05
CHEMBL4780381 — — 1 9.05
CHEMBL4798754 — — 1 9.05
CHEMBL4789322 — — 1 9.05
CHEMBL4799272 — — 1 9.00
CHEMBL4784036 — — 1 9.00
CHEMBL1231612 — — 1 9.00
CHEMBL4781149 — — 1 8.96
CHEMBL4800011 — — 1 8.96
CHEMBL4780256 — — 1 8.96
CHEMBL4798400 — — 1 8.96
CHEMBL4796443 — — 1 8.92
CHEMBL527468 — — 1 8.89
CHEMBL4781827 — — 1 8.89
CHEMBL4796554 — — 1 8.89
CHEMBL4793581 — — 1 8.85
CHEMBL4795829 — — 1 8.80
CHEMBL4797103 — — 1 8.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4780298 — Ki = 0.5 nM 9.30
CHEMBL129788 — Ki = 0.6 nM 9.22
CHEMBL4792349 — Ki = 0.6 nM 9.22
CHEMBL4781162 — Ki = 0.7 nM 9.15
CHEMBL4792035 — Ki = 0.7 nM 9.15
CHEMBL4778245 — Ki = 0.7 nM 9.15
CHEMBL4783968 — Ki = 0.8 nM 9.10
CHEMBL4784738 — Ki = 0.8 nM 9.10
CHEMBL4793034 — Ki = 0.8 nM 9.10
CHEMBL587606 — Ki = 0.8 nM 9.10
CHEMBL4795771 — Ki = 0.8 nM 9.10
CHEMBL4796933 — Ki = 0.8 nM 9.10
CHEMBL4798754 — Ki = 0.9 nM 9.05
CHEMBL4782529 — Ki = 0.9 nM 9.05
CHEMBL4780381 — Ki = 0.9 nM 9.05
CHEMBL4789322 — Ki = 0.9 nM 9.05
CHEMBL4799272 — Ki = 1.0 nM 9.00
CHEMBL4784036 — Ki = 1.0 nM 9.00
CHEMBL1231612 — Ki = 1.0 nM 9.00
CHEMBL4781149 — Ki = 1.1 nM 8.96
CHEMBL4800011 — Ki = 1.1 nM 8.96
CHEMBL4780256 — Ki = 1.1 nM 8.96
CHEMBL4798400 — Ki = 1.1 nM 8.96
CHEMBL4796443 — Ki = 1.2 nM 8.92
CHEMBL527468 — Ki = 1.3 nM 8.89
CHEMBL4796554 — Ki = 1.3 nM 8.89
CHEMBL4781827 — Ki = 1.3 nM 8.89
CHEMBL4793581 — Ki = 1.4 nM 8.85
CHEMBL4795829 — Ki = 1.6 nM 8.80
CHEMBL4797103 — Ki = 1.7 nM 8.77
CHEMBL4800362 — Ki = 1.9 nM 8.72
CHEMBL528489 — Ki = 2.0 nM 8.70
CHEMBL4798412 — Ki = 2.1 nM 8.68
CHEMBL4800635 — Ki = 2.1 nM 8.68
CHEMBL4777058 — Ki = 2.5 nM 8.60
CHEMBL4791022 — Ki = 2.6 nM 8.59
CHEMBL4796828 — Ki = 2.8 nM 8.55
CHEMBL4799632 — Ki = 2.9 nM 8.54
CHEMBL4788495 — Ki = 3.3 nM 8.48
CHEMBL4784378 — Ki = 3.6 nM 8.44
CHEMBL4798973 — Ki = 3.8 nM 8.42
CHEMBL4781350 — Ki = 4.0 nM 8.40
CHEMBL4779476 — Ki = 4.3 nM 8.37
CHEMBL4786084 — Ki = 4.7 nM 8.33
CHEMBL4789860 — Ki = 4.8 nM 8.32
CHEMBL4791594 — Ki = 5.2 nM 8.28
CHEMBL4786930 — Ki = 6.4 nM 8.19
CHEMBL4789386 — Ki = 9.85 nM 8.01
CHEMBL747 CYCLOGUANIL Ki = 43.2 nM 7.37