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Assay Detail

CHEMBL3996774

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Functional
Anti-plasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by [3H]-hypoxanthine incorporation assay
ChEMBL ↗
62
Total Activities
62
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

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.
Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K.
J Med Chem (2017) 60 : 1432 -1448
PubMed 28094524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 6.14 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097733 — — 1 7.70
CHEMBL4095280 — — 1 7.52
CHEMBL4068923 — — 1 7.52
CHEMBL4093636 — — 1 7.40
CHEMBL4090006 — — 1 7.30
CHEMBL4087580 — — 1 7.16
CHEMBL4062856 — — 1 6.96
CHEMBL1800559 — — 1 6.92
CHEMBL4084045 — — 1 6.85
CHEMBL4105454 — — 1 6.85
CHEMBL4079700 — — 1 6.82
CHEMBL4092272 — — 1 6.77
CHEMBL4082152 — — 1 6.75
CHEMBL4081540 — — 1 6.72
CHEMBL4100993 — — 1 6.68
CHEMBL4060251 — — 1 6.58
CHEMBL4062329 — — 1 6.57
CHEMBL4061812 — — 1 6.51
CHEMBL4097620 — — 1 6.48
CHEMBL4079203 — — 1 6.44
CHEMBL4067864 — — 1 6.42
CHEMBL4084534 — — 1 6.42
CHEMBL4085896 — — 1 6.41
CHEMBL4070265 — — 1 6.36
CHEMBL4070434 — — 1 6.33
CHEMBL4099549 — — 1 6.26
CHEMBL4074246 — — 1 6.18
CHEMBL4065621 — — 1 6.16
CHEMBL4071316 — — 1 6.16
CHEMBL4089718 — — 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097733 — IC50 = 20.0 nM 7.70
CHEMBL4095280 — IC50 = 30.0 nM 7.52
CHEMBL4068923 — IC50 = 30.0 nM 7.52
CHEMBL4093636 — IC50 = 40.0 nM 7.40
CHEMBL4090006 — IC50 = 50.0 nM 7.30
CHEMBL4087580 — IC50 = 70.0 nM 7.16
CHEMBL4062856 — IC50 = 110.0 nM 6.96
CHEMBL1800559 — IC50 = 120.0 nM 6.92
CHEMBL4084045 — IC50 = 140.0 nM 6.85
CHEMBL4105454 — IC50 = 140.0 nM 6.85
CHEMBL4079700 — IC50 = 150.0 nM 6.82
CHEMBL4092272 — IC50 = 170.0 nM 6.77
CHEMBL4082152 — IC50 = 180.0 nM 6.75
CHEMBL4081540 — IC50 = 190.0 nM 6.72
CHEMBL4100993 — IC50 = 210.0 nM 6.68
CHEMBL4060251 — IC50 = 260.0 nM 6.58
CHEMBL4062329 — IC50 = 270.0 nM 6.57
CHEMBL4061812 — IC50 = 310.0 nM 6.51
CHEMBL4097620 — IC50 = 330.0 nM 6.48
CHEMBL4079203 — IC50 = 360.0 nM 6.44
CHEMBL4067864 — IC50 = 380.0 nM 6.42
CHEMBL4084534 — IC50 = 380.0 nM 6.42
CHEMBL4085896 — IC50 = 390.0 nM 6.41
CHEMBL4070265 — IC50 = 440.0 nM 6.36
CHEMBL4070434 — IC50 = 470.0 nM 6.33
CHEMBL4099549 — IC50 = 550.0 nM 6.26
CHEMBL4074246 — IC50 = 660.0 nM 6.18
CHEMBL4065621 — IC50 = 700.0 nM 6.16
CHEMBL4071316 — IC50 = 690.0 nM 6.16
CHEMBL4089718 — IC50 = 700.0 nM 6.16
CHEMBL4097609 — IC50 = 830.0 nM 6.08
CHEMBL4088794 — IC50 = 840.0 nM 6.08
CHEMBL4070446 — IC50 = 890.0 nM 6.05
CHEMBL4084546 — IC50 = 950.0 nM 6.02
CHEMBL4072933 — IC50 = 1100.0 nM 5.96
CHEMBL4089743 — IC50 = 1140.0 nM 5.94
CHEMBL4073686 — IC50 = 1280.0 nM 5.89
CHEMBL4061601 — IC50 = 1380.0 nM 5.86
CHEMBL4071478 — IC50 = 1560.0 nM 5.81
CHEMBL4089873 — IC50 = 2930.0 nM 5.53
CHEMBL4071489 — IC50 = 3000.0 nM 5.52
CHEMBL4082011 — IC50 = 3810.0 nM 5.42
CHEMBL4100022 — IC50 = 3900.0 nM 5.41
CHEMBL4099858 — IC50 = 4130.0 nM 5.38
CHEMBL4067555 — IC50 = 4420.0 nM 5.36
CHEMBL4059963 — IC50 = 4960.0 nM 5.30
CHEMBL4089645 — IC50 = 5020.0 nM 5.30
CHEMBL4100503 — IC50 = 5530.0 nM 5.26
CHEMBL4064354 — IC50 = 5990.0 nM 5.22
CHEMBL4068621 — IC50 = 6450.0 nM 5.19