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Assay Detail

CHEMBL4768940

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

Functional
Antimalarial activity against Plasmodium falciparum TM4/8.2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured after 20 hrs by radioactivity method
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364) ↗
Type ORGANISM
Organism Plasmodium falciparum

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
IC50 49 7.64 10.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782529 — — 1 10.47
CHEMBL4780381 — — 1 9.55
CHEMBL1231612 — — 1 9.46
CHEMBL4784036 — — 1 9.43
CHEMBL4798400 — — 1 9.32
CHEMBL4799272 — — 1 9.28
CHEMBL587606 — — 1 9.28
CHEMBL129788 — — 1 9.24
CHEMBL4789322 — — 1 9.22
CHEMBL4792349 — — 1 8.89
CHEMBL4795771 — — 1 8.89
CHEMBL4793581 — — 1 8.77
CHEMBL4780298 — — 1 8.64
CHEMBL527468 — — 1 8.54
CHEMBL4780256 — — 1 8.48
CHEMBL4796933 — — 1 8.46
CHEMBL4784738 — — 1 8.35
CHEMBL4800362 — — 1 8.29
CHEMBL4796554 — — 1 8.04
CHEMBL4800011 — — 1 7.92
CHEMBL4781827 — — 1 7.85
CHEMBL4798754 — — 1 7.70
CHEMBL4799632 — — 1 7.66
CHEMBL4792035 — — 1 7.64
CHEMBL4797103 — — 1 7.62
CHEMBL4781149 — — 1 7.58
CHEMBL4800635 — — 1 7.58
CHEMBL4791022 — — 1 7.54
CHEMBL4781162 — — 1 7.52
CHEMBL528489 — — 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782529 — IC50 = 0.034 nM 10.47
CHEMBL4780381 — IC50 = 0.28 nM 9.55
CHEMBL1231612 — IC50 = 0.35 nM 9.46
CHEMBL4784036 — IC50 = 0.37 nM 9.43
CHEMBL4798400 — IC50 = 0.48 nM 9.32
CHEMBL4799272 — IC50 = 0.52 nM 9.28
CHEMBL587606 — IC50 = 0.52 nM 9.28
CHEMBL129788 — IC50 = 0.57 nM 9.24
CHEMBL4789322 — IC50 = 0.6 nM 9.22
CHEMBL4792349 — IC50 = 1.3 nM 8.89
CHEMBL4795771 — IC50 = 1.3 nM 8.89
CHEMBL4793581 — IC50 = 1.7 nM 8.77
CHEMBL4780298 — IC50 = 2.3 nM 8.64
CHEMBL527468 — IC50 = 2.9 nM 8.54
CHEMBL4780256 — IC50 = 3.3 nM 8.48
CHEMBL4796933 — IC50 = 3.5 nM 8.46
CHEMBL4784738 — IC50 = 4.5 nM 8.35
CHEMBL4800362 — IC50 = 5.1 nM 8.29
CHEMBL4796554 — IC50 = 9.2 nM 8.04
CHEMBL4800011 — IC50 = 12.0 nM 7.92
CHEMBL4781827 — IC50 = 14.0 nM 7.85
CHEMBL4798754 — IC50 = 20.0 nM 7.70
CHEMBL4799632 — IC50 = 22.0 nM 7.66
CHEMBL4792035 — IC50 = 23.0 nM 7.64
CHEMBL4797103 — IC50 = 24.0 nM 7.62
CHEMBL4800635 — IC50 = 26.0 nM 7.58
CHEMBL4781149 — IC50 = 26.0 nM 7.58
CHEMBL4791022 — IC50 = 29.0 nM 7.54
CHEMBL4781162 — IC50 = 30.0 nM 7.52
CHEMBL528489 — IC50 = 30.0 nM 7.52
CHEMBL4783968 — IC50 = 31.0 nM 7.51
CHEMBL4778245 — IC50 = 33.0 nM 7.48
CHEMBL747 CYCLOGUANIL IC50 = 37.0 nM 7.43
CHEMBL4779476 — IC50 = 51.0 nM 7.29
CHEMBL4788495 — IC50 = 80.0 nM 7.10
CHEMBL4795829 — IC50 = 150.0 nM 6.82
CHEMBL4777058 — IC50 = 400.0 nM 6.40
CHEMBL4781350 — IC50 = 440.0 nM 6.36
CHEMBL4798412 — IC50 = 750.0 nM 6.12
CHEMBL4796443 — IC50 = 750.0 nM 6.12
CHEMBL4786084 — IC50 = 1200.0 nM 5.92
CHEMBL4793034 — IC50 = 1850.0 nM 5.73
CHEMBL4791594 — IC50 = 1900.0 nM 5.72
CHEMBL4786930 — IC50 = 2000.0 nM 5.70
CHEMBL4789386 — IC50 = 2200.0 nM 5.66
CHEMBL4784378 — IC50 = 2400.0 nM 5.62
CHEMBL4796828 — IC50 = 2670.0 nM 5.57
CHEMBL4798973 — IC50 = 3000.0 nM 5.52
CHEMBL4789860 — IC50 = 4400.0 nM 5.36