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Assay Detail

CHEMBL3296130

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

Functional
Antiplasmodial activity against Plasmodium falciparum Dd2 harboring DHODH mutant
5
Total Activities
5
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

Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.
Hameed P S, Chinnapattu M, Shanbag G, Manjrekar P, Koushik K, Raichurkar A, Patil V, Jatheendranath S, Rudrapatna SS, Barde SP, Rautela N, Awasthy D, Morayya S, Narayan C, Kavanagh S, Saralaya R, Bharath S, Viswanath P, Mukherjee K, Bandodkar B, Srivastava A, Panduga V, Reddy J, Prabhakar KR, Sinha A, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Magistrado PA, Lukens AK, Wirth DF, Waterson D, Balasubramanian V, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK, Ramachandran S.
J Med Chem (2014) 57 : 5702 -5713
PubMed 24914738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.59 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 8.74
CHEMBL1706506 1 7.77
CHEMBL3289810 1 7.71
CHEMBL2012958 1 7.12
CHEMBL278315 GELDANAMYCIN 2.0 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ IC50 = 1.81 nM 8.74
CHEMBL1706506 IC50 = 16.9 nM 7.77
CHEMBL3289810 IC50 = 19.72 nM 7.71
CHEMBL2012958 IC50 = 76.8 nM 7.12
CHEMBL278315 GELDANAMYCIN IC50 = 257.0 nM 6.59