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Assay Detail

CHEMBL4768942

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Functional
Antimalarial activity against Plasmodium falciparum K1CB1 harboring DHFR C59R/S108T mutant 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
Cell Type Erythrocyte
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 6.92 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782529 — — 1 9.59
CHEMBL4780381 — — 1 8.72
CHEMBL1231612 — — 1 8.72
CHEMBL129788 — — 1 8.64
CHEMBL4798400 — — 1 8.44
CHEMBL587606 — — 1 8.32
CHEMBL4792035 — — 1 8.28
CHEMBL4784036 — — 1 8.27
CHEMBL4795771 — — 1 8.26
CHEMBL4792349 — — 1 8.23
CHEMBL4789322 — — 1 8.21
CHEMBL4780298 — — 1 7.72
CHEMBL4796554 — — 1 7.66
CHEMBL4781162 — — 1 7.54
CHEMBL4778245 — — 1 7.51
CHEMBL4797103 — — 1 7.50
CHEMBL4799272 — — 1 7.50
CHEMBL527468 — — 1 7.48
CHEMBL4800635 — — 1 7.46
CHEMBL4796933 — — 1 7.43
CHEMBL528489 — — 1 7.41
CHEMBL4800362 — — 1 7.36
CHEMBL4784738 — — 1 7.35
CHEMBL4781827 — — 1 7.32
CHEMBL4793581 — — 1 7.31
CHEMBL4800011 — — 1 7.07
CHEMBL4781149 — — 1 7.00
CHEMBL4798754 — — 1 6.72
CHEMBL4791022 — — 1 6.64
CHEMBL4793034 — — 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782529 — IC50 = 0.26 nM 9.59
CHEMBL4780381 — IC50 = 1.9 nM 8.72
CHEMBL1231612 — IC50 = 1.9 nM 8.72
CHEMBL129788 — IC50 = 2.3 nM 8.64
CHEMBL4798400 — IC50 = 3.6 nM 8.44
CHEMBL587606 — IC50 = 4.8 nM 8.32
CHEMBL4792035 — IC50 = 5.2 nM 8.28
CHEMBL4784036 — IC50 = 5.4 nM 8.27
CHEMBL4795771 — IC50 = 5.5 nM 8.26
CHEMBL4792349 — IC50 = 5.9 nM 8.23
CHEMBL4789322 — IC50 = 6.1 nM 8.21
CHEMBL4780298 — IC50 = 19.0 nM 7.72
CHEMBL4796554 — IC50 = 22.0 nM 7.66
CHEMBL4781162 — IC50 = 29.0 nM 7.54
CHEMBL4778245 — IC50 = 31.0 nM 7.51
CHEMBL4797103 — IC50 = 32.0 nM 7.50
CHEMBL4799272 — IC50 = 32.0 nM 7.50
CHEMBL527468 — IC50 = 33.0 nM 7.48
CHEMBL4800635 — IC50 = 35.0 nM 7.46
CHEMBL4796933 — IC50 = 37.0 nM 7.43
CHEMBL528489 — IC50 = 39.0 nM 7.41
CHEMBL4800362 — IC50 = 44.0 nM 7.36
CHEMBL4784738 — IC50 = 45.0 nM 7.35
CHEMBL4781827 — IC50 = 48.0 nM 7.32
CHEMBL4793581 — IC50 = 49.0 nM 7.31
CHEMBL4800011 — IC50 = 85.0 nM 7.07
CHEMBL4781149 — IC50 = 100.0 nM 7.00
CHEMBL4798754 — IC50 = 190.0 nM 6.72
CHEMBL4791022 — IC50 = 230.0 nM 6.64
CHEMBL4793034 — IC50 = 240.0 nM 6.62
CHEMBL4780256 — IC50 = 260.0 nM 6.58
CHEMBL4799632 — IC50 = 350.0 nM 6.46
CHEMBL4783968 — IC50 = 400.0 nM 6.40
CHEMBL4796443 — IC50 = 490.0 nM 6.31
CHEMBL4784378 — IC50 = 530.0 nM 6.28
CHEMBL4796828 — IC50 = 1800.0 nM 5.75
CHEMBL4795829 — IC50 = 2300.0 nM 5.64
CHEMBL747 CYCLOGUANIL IC50 = 2400.0 nM 5.62
CHEMBL4777058 — IC50 = 2400.0 nM 5.62
CHEMBL4798412 — IC50 = 2900.0 nM 5.54
CHEMBL4789386 — IC50 = 3100.0 nM 5.51
CHEMBL4798973 — IC50 = 4000.0 nM 5.40
CHEMBL4779476 — IC50 = 5400.0 nM 5.27
CHEMBL4786084 — IC50 = 5900.0 nM 5.23
CHEMBL4791594 — IC50 = 7200.0 nM 5.14
CHEMBL4781350 — IC50 = 9600.0 nM 5.02
CHEMBL4786930 — IC50 = 9700.0 nM 5.01
CHEMBL4789860 — IC50 = 10000.0 nM 5.00
CHEMBL4788495 — IC50 = 16200.0 nM 4.79