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Assay Detail

CHEMBL1016138

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

Functional
Antiplasmodial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake
40
Total Activities
40
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

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice.
Gujjar R, Marwaha A, El Mazouni F, White J, White KL, Creason S, Shackleford DM, Baldwin J, Charman WN, Buckner FS, Charman S, Rathod PK, Phillips MA.
J Med Chem (2009) 52 : 1864 -1872
PubMed 19296651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 5.07 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492529 1 6.47
CHEMBL492720 1 5.89
CHEMBL13380 1 5.58
CHEMBL492719 1 5.44
CHEMBL492530 1 5.42
CHEMBL492520 1 5.38
CHEMBL447995 1 5.32
CHEMBL492549 1 5.30
CHEMBL492528 1 5.19
CHEMBL437480 1 5.09
CHEMBL492336 1 5.09
CHEMBL499296 1 5.07
CHEMBL492712 1 5.06
CHEMBL522325 1 5.06
CHEMBL452465 1 4.92
CHEMBL523669 1 4.85
CHEMBL474842 1 4.72
CHEMBL452667 1 4.60
CHEMBL454269 1 4.52
CHEMBL514038 1 4.47
CHEMBL502389 1 4.46
CHEMBL475664 1 4.43
CHEMBL474004 1 4.30
CHEMBL452392 1 -
CHEMBL444928 1 -
CHEMBL492711 1 -
CHEMBL492695 1 -
CHEMBL451525 1 -
CHEMBL523163 1 -
CHEMBL492497 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492529 EC50 = 340.0 nM 6.47
CHEMBL492720 EC50 = 1300.0 nM 5.89
CHEMBL13380 EC50 = 2600.0 nM 5.58
CHEMBL492719 EC50 = 3600.0 nM 5.44
CHEMBL492530 EC50 = 3800.0 nM 5.42
CHEMBL492520 EC50 = 4200.0 nM 5.38
CHEMBL447995 EC50 = 4800.0 nM 5.32
CHEMBL492549 EC50 = 5000.0 nM 5.30
CHEMBL492528 EC50 = 6400.0 nM 5.19
CHEMBL437480 EC50 = 8100.0 nM 5.09
CHEMBL492336 EC50 = 8200.0 nM 5.09
CHEMBL499296 EC50 = 8500.0 nM 5.07
CHEMBL492712 EC50 = 8700.0 nM 5.06
CHEMBL522325 EC50 = 8800.0 nM 5.06
CHEMBL452465 EC50 = 12000.0 nM 4.92
CHEMBL523669 EC50 = 14000.0 nM 4.85
CHEMBL474842 EC50 = 19000.0 nM 4.72
CHEMBL452667 EC50 = 25000.0 nM 4.60
CHEMBL454269 EC50 = 30000.0 nM 4.52
CHEMBL514038 EC50 = 34000.0 nM 4.47
CHEMBL502389 EC50 = 35000.0 nM 4.46
CHEMBL475664 EC50 = 37000.0 nM 4.43
CHEMBL474004 EC50 = 50000.0 nM 4.30
CHEMBL473816 EC50 > 50000.0 nM -
CHEMBL475663 EC50 - -
CHEMBL500504 EC50 - -
CHEMBL522991 EC50 > 50000.0 nM -
CHEMBL506446 EC50 - -
CHEMBL492550 EC50 > 50000.0 nM -
CHEMBL493761 EC50 > 50000.0 nM -
CHEMBL451417 EC50 > 50000.0 nM -
CHEMBL523691 EC50 - -
CHEMBL508404 EC50 > 50000.0 nM -
CHEMBL492497 EC50 > 50000.0 nM -
CHEMBL523163 EC50 > 50000.0 nM -
CHEMBL451525 EC50 > 50000.0 nM -
CHEMBL492695 EC50 - -
CHEMBL492711 EC50 > 5000.0 nM -
CHEMBL444928 EC50 > 50000.0 nM -
CHEMBL452392 EC50 > 5000.0 nM -