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

CHEMBL5160032

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

Functional
Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as inhibition of parasite growth by SYBR Green-I dye based fluorescence analysis
68
Total Activities
59
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

Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Taft BR, Yokokawa F, Kirrane T, Mata AC, Huang R, Blaquiere N, Waldron G, Zou B, Simon O, Vankadara S, Chan WL, Ding M, Sim S, Straimer J, Guiguemde A, Lakshminarayana SB, Jain JP, Bodenreider C, Thompson C, Lanshoeft C, Shu W, Fang E, Qumber J, Chan K, Pei L, Chen YL, Schulz H, Lim J, Abas SN, Ang X, Liu Y, Angulo-Barturen I, Jiménez-Díaz MB, Gamo FJ, Crespo-Fernandez B, Rosenthal PJ, Cooper RA, Tumwebaze P, Aguiar ACC, Campo B, Campbell S, Wagner J, Diagana TT, Sarko C.
J Med Chem (2022) 65 : 3798 -3813
PubMed 35229610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 68 7.26 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5200418 1 8.30
CHEMBL5173264 INE-963 2.0 1 8.22
CHEMBL5201780 1 8.05
CHEMBL5173325 1 8.05
CHEMBL5174770 1 7.96
CHEMBL5196893 1 7.89
CHEMBL5207627 1 7.85
CHEMBL5173722 1 7.85
CHEMBL5199435 1 7.77
CHEMBL5189523 1 7.77
CHEMBL5174065 1 7.77
CHEMBL5181699 1 7.77
CHEMBL5185965 2 7.70
CHEMBL5192443 1 7.70
CHEMBL5198037 2 7.70
CHEMBL5181112 1 7.68
CHEMBL5201904 1 7.68
CHEMBL5189070 1 7.66
CHEMBL5200247 1 7.66
CHEMBL5178777 2 7.62
CHEMBL5179988 1 7.60
CHEMBL5190339 2 7.58
CHEMBL5204715 1 7.55
CHEMBL5187610 1 7.55
CHEMBL5169763 2 7.54
CHEMBL5187946 2 7.54
CHEMBL5197907 2 7.51
CHEMBL5175200 1 7.48
CHEMBL172 (S,R)-MEFLOQUINE 1 7.47
CHEMBL5193817 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5200418 EC50 = 5.0 nM 8.30
CHEMBL5173264 INE-963 EC50 = 6.0 nM 8.22
CHEMBL5201780 EC50 = 9.0 nM 8.05
CHEMBL5173325 EC50 = 9.0 nM 8.05
CHEMBL5174770 EC50 = 11.0 nM 7.96
CHEMBL5196893 EC50 = 13.0 nM 7.89
CHEMBL5173722 EC50 = 14.0 nM 7.85
CHEMBL5207627 EC50 = 14.0 nM 7.85
CHEMBL5174065 EC50 = 17.0 nM 7.77
CHEMBL5189523 EC50 = 17.0 nM 7.77
CHEMBL5199435 EC50 = 17.0 nM 7.77
CHEMBL5181699 EC50 = 17.0 nM 7.77
CHEMBL5185965 EC50 = 20.0 nM 7.70
CHEMBL5198037 EC50 = 20.0 nM 7.70
CHEMBL5185965 EC50 = 20.0 nM 7.70
CHEMBL5192443 EC50 = 20.0 nM 7.70
CHEMBL5198037 EC50 = 21.0 nM 7.68
CHEMBL5181112 EC50 = 21.0 nM 7.68
CHEMBL5201904 EC50 = 21.0 nM 7.68
CHEMBL5200247 EC50 = 22.0 nM 7.66
CHEMBL5189070 EC50 = 22.0 nM 7.66
CHEMBL5178777 EC50 = 24.0 nM 7.62
CHEMBL5179988 EC50 = 25.0 nM 7.60
CHEMBL5190339 EC50 = 26.0 nM 7.58
CHEMBL5178777 EC50 = 27.0 nM 7.57
CHEMBL5204715 EC50 = 28.0 nM 7.55
CHEMBL5190339 EC50 = 28.0 nM 7.55
CHEMBL5187610 EC50 = 28.0 nM 7.55
CHEMBL5169763 EC50 = 29.0 nM 7.54
CHEMBL5169763 EC50 = 29.0 nM 7.54
CHEMBL5187946 EC50 = 29.0 nM 7.54
CHEMBL5197907 EC50 = 31.0 nM 7.51
CHEMBL5175200 EC50 = 33.0 nM 7.48
CHEMBL172 (S,R)-MEFLOQUINE EC50 = 34.0 nM 7.47
CHEMBL5197907 EC50 = 38.0 nM 7.42
CHEMBL5193817 EC50 = 44.0 nM 7.36
CHEMBL5187817 EC50 = 45.0 nM 7.35
CHEMBL5206310 EC50 = 45.0 nM 7.35
CHEMBL5178067 EC50 = 45.0 nM 7.35
CHEMBL5187946 EC50 = 46.0 nM 7.34
CHEMBL5195201 EC50 = 52.0 nM 7.28
CHEMBL5172261 EC50 = 53.0 nM 7.28
CHEMBL5188137 EC50 = 56.0 nM 7.25
CHEMBL5206260 EC50 = 62.0 nM 7.21
CHEMBL5187715 EC50 = 62.0 nM 7.21
CHEMBL5178067 EC50 = 66.0 nM 7.18
CHEMBL5187715 EC50 = 67.0 nM 7.17
CHEMBL5189235 EC50 = 67.0 nM 7.17
CHEMBL5191906 EC50 = 79.0 nM 7.10
CHEMBL5197359 EC50 = 82.0 nM 7.09