Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL767132

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

Functional
In vitro antiplasmodial activity (IC50) against Plasmodium falciparum wtTM4/8.2
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364) ↗
Type ORGANISM
Organism Plasmodium falciparum

Publication

Development of 2,4-diaminopyrimidines as antimalarials based on inhibition of the S108N and C59R+S108N mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparum.
Tarnchompoo B, Sirichaiwat C, Phupong W, Intaraudom C, Sirawaraporn W, Kamchonwongpaisan S, Vanichtanankul J, Thebtaranonth Y, Yuthavong Y.
J Med Chem (2002) 45 : 1244 -1252
PubMed 11881993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.07 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22405 — — 1 7.40
CHEMBL282275 — — 1 7.30
CHEMBL21691 — — 1 7.30
CHEMBL21799 ETOPRINE -1.0 1 7.22
CHEMBL416552 — — 1 7.22
CHEMBL22901 — — 1 7.16
CHEMBL36 PYRIMETHAMINE 4.0 1 7.10
CHEMBL21778 — — 1 7.00
CHEMBL22139 — — 1 6.82
CHEMBL22693 — — 1 6.70
CHEMBL281412 — — 1 6.52
CHEMBL22811 — — 1 6.52
CHEMBL278813 — — 1 6.40
CHEMBL21407 — — 1 6.40
CHEMBL278847 — — 1 6.40
CHEMBL22403 — — 1 6.40
CHEMBL434771 — — 1 6.40
CHEMBL416373 — — 1 6.36
CHEMBL21357 — — 1 6.30
CHEMBL21395 — — 1 6.30
CHEMBL21885 — — 1 6.22
CHEMBL21921 — — 1 6.16
CHEMBL416376 — — 1 6.16
CHEMBL22148 — — 1 6.16
CHEMBL21494 — — 1 6.10
CHEMBL279492 — — 1 5.64
CHEMBL22039 — — 1 5.62
CHEMBL22327 — — 1 5.52
CHEMBL25112 — — 1 5.52
CHEMBL22138 — — 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22405 — IC50 = 40.0 nM 7.40
CHEMBL282275 — IC50 = 50.0 nM 7.30
CHEMBL21691 — IC50 = 50.0 nM 7.30
CHEMBL21799 ETOPRINE IC50 = 60.0 nM 7.22
CHEMBL416552 — IC50 = 60.0 nM 7.22
CHEMBL22901 — IC50 = 70.0 nM 7.16
CHEMBL36 PYRIMETHAMINE IC50 = 80.0 nM 7.10
CHEMBL21778 — IC50 = 100.0 nM 7.00
CHEMBL22139 — IC50 = 150.0 nM 6.82
CHEMBL22693 — IC50 = 200.0 nM 6.70
CHEMBL22811 — IC50 = 300.0 nM 6.52
CHEMBL281412 — IC50 = 300.0 nM 6.52
CHEMBL434771 — IC50 = 400.0 nM 6.40
CHEMBL22403 — IC50 = 400.0 nM 6.40
CHEMBL278847 — IC50 = 400.0 nM 6.40
CHEMBL278813 — IC50 = 400.0 nM 6.40
CHEMBL21407 — IC50 = 400.0 nM 6.40
CHEMBL416373 — IC50 = 440.0 nM 6.36
CHEMBL21357 — IC50 = 500.0 nM 6.30
CHEMBL21395 — IC50 = 500.0 nM 6.30
CHEMBL21885 — IC50 = 600.0 nM 6.22
CHEMBL21921 — IC50 = 700.0 nM 6.16
CHEMBL22148 — IC50 = 700.0 nM 6.16
CHEMBL416376 — IC50 = 700.0 nM 6.16
CHEMBL21494 — IC50 = 800.0 nM 6.10
CHEMBL279492 — IC50 = 2300.0 nM 5.64
CHEMBL22039 — IC50 = 2400.0 nM 5.62
CHEMBL22327 — IC50 = 3000.0 nM 5.52
CHEMBL25112 — IC50 = 3000.0 nM 5.52
CHEMBL22138 — IC50 = 3100.0 nM 5.51
CHEMBL22137 — IC50 = 3600.0 nM 5.44
CHEMBL22271 — IC50 = 3700.0 nM 5.43
CHEMBL22129 — IC50 = 3700.0 nM 5.43
CHEMBL279509 — IC50 = 4200.0 nM 5.38
CHEMBL279948 — IC50 = 4500.0 nM 5.35
CHEMBL22146 — IC50 = 4700.0 nM 5.33
CHEMBL21414 — IC50 = 6000.0 nM 5.22
CHEMBL22 TRIMETHOPRIM IC50 = 6700.0 nM 5.17
CHEMBL21408 — IC50 = 7400.0 nM 5.13
CHEMBL22357 — IC50 = 11300.0 nM 4.95
CHEMBL279986 — IC50 = 13100.0 nM 4.88
CHEMBL280410 — IC50 = 19000.0 nM 4.72
CHEMBL21690 — IC50 = 20900.0 nM 4.68