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Assay Detail

CHEMBL4768944

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Functional
Antimalarial activity against Plasmodium falciparum CsI-2 harboring DHFR C59R/S108N/I164L 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 6.26 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782529 — — 1 8.51
CHEMBL129788 — — 1 8.42
CHEMBL4780381 — — 1 8.41
CHEMBL1231612 — — 1 8.41
CHEMBL4798400 — — 1 8.36
CHEMBL4796933 — — 1 7.50
CHEMBL4784036 — — 1 7.50
CHEMBL4789322 — — 1 7.43
CHEMBL587606 — — 1 7.41
CHEMBL4795771 — — 1 7.38
CHEMBL4800635 — — 1 7.34
CHEMBL4778245 — — 1 7.34
CHEMBL4792035 — — 1 7.33
CHEMBL4780298 — — 1 7.32
CHEMBL4792349 — — 1 7.21
CHEMBL4797103 — — 1 6.85
CHEMBL4799272 — — 1 6.85
CHEMBL4793581 — — 1 6.77
CHEMBL527468 — — 1 6.66
CHEMBL4796554 — — 1 6.60
CHEMBL4780256 — — 1 6.58
CHEMBL528489 — — 1 6.52
CHEMBL4781149 — — 1 6.51
CHEMBL4800362 — — 1 6.47
CHEMBL4781162 — — 1 6.42
CHEMBL4784738 — — 1 6.41
CHEMBL4781827 — — 1 6.40
CHEMBL4799632 — — 1 6.30
CHEMBL4800011 — — 1 6.14
CHEMBL4791022 — — 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782529 — IC50 = 3.1 nM 8.51
CHEMBL129788 — IC50 = 3.8 nM 8.42
CHEMBL1231612 — IC50 = 3.9 nM 8.41
CHEMBL4780381 — IC50 = 3.9 nM 8.41
CHEMBL4798400 — IC50 = 4.4 nM 8.36
CHEMBL4796933 — IC50 = 32.0 nM 7.50
CHEMBL4784036 — IC50 = 32.0 nM 7.50
CHEMBL4789322 — IC50 = 37.0 nM 7.43
CHEMBL587606 — IC50 = 39.0 nM 7.41
CHEMBL4795771 — IC50 = 42.0 nM 7.38
CHEMBL4800635 — IC50 = 46.0 nM 7.34
CHEMBL4778245 — IC50 = 46.0 nM 7.34
CHEMBL4792035 — IC50 = 47.0 nM 7.33
CHEMBL4780298 — IC50 = 48.0 nM 7.32
CHEMBL4792349 — IC50 = 62.0 nM 7.21
CHEMBL4797103 — IC50 = 140.0 nM 6.85
CHEMBL4799272 — IC50 = 140.0 nM 6.85
CHEMBL4793581 — IC50 = 170.0 nM 6.77
CHEMBL527468 — IC50 = 220.0 nM 6.66
CHEMBL4796554 — IC50 = 250.0 nM 6.60
CHEMBL4780256 — IC50 = 260.0 nM 6.58
CHEMBL528489 — IC50 = 300.0 nM 6.52
CHEMBL4781149 — IC50 = 310.0 nM 6.51
CHEMBL4800362 — IC50 = 340.0 nM 6.47
CHEMBL4781162 — IC50 = 380.0 nM 6.42
CHEMBL4784738 — IC50 = 390.0 nM 6.41
CHEMBL4781827 — IC50 = 400.0 nM 6.40
CHEMBL4799632 — IC50 = 500.0 nM 6.30
CHEMBL4800011 — IC50 = 720.0 nM 6.14
CHEMBL4791022 — IC50 = 2400.0 nM 5.62
CHEMBL4783968 — IC50 = 3100.0 nM 5.51
CHEMBL4798412 — IC50 = 3100.0 nM 5.51
CHEMBL4793034 — IC50 = 3200.0 nM 5.50
CHEMBL4796443 — IC50 = 3300.0 nM 5.48
CHEMBL4789386 — IC50 = 3500.0 nM 5.46
CHEMBL4784378 — IC50 = 3600.0 nM 5.44
CHEMBL4798754 — IC50 = 4500.0 nM 5.35
CHEMBL4777058 — IC50 = 4800.0 nM 5.32
CHEMBL4795829 — IC50 = 5000.0 nM 5.30
CHEMBL4798973 — IC50 = 7900.0 nM 5.10
CHEMBL4791594 — IC50 = 17100.0 nM 4.77
CHEMBL4788495 — IC50 = 20500.0 nM 4.69
CHEMBL4786084 — IC50 = 25300.0 nM 4.60
CHEMBL4781350 — IC50 = 31200.0 nM 4.51
CHEMBL747 CYCLOGUANIL IC50 = 37900.0 nM 4.42
CHEMBL4796828 — IC50 = 47600.0 nM 4.32
CHEMBL4786930 — IC50 = 63300.0 nM 4.20
CHEMBL4779476 — IC50 = 73400.0 nM 4.13
CHEMBL4789860 — IC50 = 76500.0 nM 4.12