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Assay Detail

CHEMBL4835667

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Functional
Antimalarial activity against asexual blood stage drug-sensitive Plasmodium falciparum NF54 infected in erythrocytes assessed as reduction in parasitemia incubated up to 72 hrs by [3H]hypoxanthine incorporation assay
ChEMBL ↗
42
Total Activities
42
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 Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure-Activity Relationship and <i>In Vivo</i> Oral Efficacy Studies.
Dziwornu GA, Coertzen D, Leshabane M, Korkor CM, Cloete CK, Njoroge M, Gibhard L, Lawrence N, Reader J, van der Watt M, Wittlin S, Birkholtz LM, Chibale K, Chibale K.
J Med Chem (2021) 64 : 5198 -5215
PubMed 33844521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.40 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 8.00
CHEMBL4874844 — — 1 7.10
CHEMBL4853530 — — 1 6.82
CHEMBL4851058 — — 1 6.82
CHEMBL4846075 — — 1 6.77
CHEMBL4865588 — — 1 6.72
CHEMBL4862272 — — 1 6.72
CHEMBL4851068 — — 1 6.72
CHEMBL4859244 — — 1 6.70
CHEMBL4851661 — — 1 6.66
CHEMBL4851055 — — 1 6.64
CHEMBL4869041 — — 1 6.60
CHEMBL4870469 — — 1 6.60
CHEMBL4853001 — — 1 6.58
CHEMBL4879028 — — 1 6.58
CHEMBL4858906 — — 1 6.58
CHEMBL4870248 — — 1 6.57
CHEMBL4879051 — — 1 6.55
CHEMBL4873489 — — 1 6.55
CHEMBL4857300 — — 1 6.52
CHEMBL4871841 — — 1 6.44
CHEMBL4876226 — — 1 6.43
CHEMBL4863267 — — 1 6.41
CHEMBL4869087 — — 1 6.40
CHEMBL4861409 — — 1 6.36
CHEMBL4849845 — — 1 6.33
CHEMBL4852597 — — 1 6.33
CHEMBL4873869 — — 1 6.26
CHEMBL4865127 — — 1 6.25
CHEMBL4846549 — — 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 10.0 nM 8.00
CHEMBL4874844 — IC50 = 80.0 nM 7.10
CHEMBL4851058 — IC50 = 150.0 nM 6.82
CHEMBL4853530 — IC50 = 150.0 nM 6.82
CHEMBL4846075 — IC50 = 170.0 nM 6.77
CHEMBL4865588 — IC50 = 190.0 nM 6.72
CHEMBL4862272 — IC50 = 190.0 nM 6.72
CHEMBL4851068 — IC50 = 190.0 nM 6.72
CHEMBL4859244 — IC50 = 200.0 nM 6.70
CHEMBL4851661 — IC50 = 220.0 nM 6.66
CHEMBL4851055 — IC50 = 230.0 nM 6.64
CHEMBL4870469 — IC50 = 250.0 nM 6.60
CHEMBL4869041 — IC50 = 250.0 nM 6.60
CHEMBL4858906 — IC50 = 260.0 nM 6.58
CHEMBL4879028 — IC50 = 260.0 nM 6.58
CHEMBL4853001 — IC50 = 260.0 nM 6.58
CHEMBL4870248 — IC50 = 270.0 nM 6.57
CHEMBL4879051 — IC50 = 280.0 nM 6.55
CHEMBL4873489 — IC50 = 280.0 nM 6.55
CHEMBL4857300 — IC50 = 300.0 nM 6.52
CHEMBL4871841 — IC50 = 360.0 nM 6.44
CHEMBL4876226 — IC50 = 370.0 nM 6.43
CHEMBL4863267 — IC50 = 390.0 nM 6.41
CHEMBL4869087 — IC50 = 400.0 nM 6.40
CHEMBL4861409 — IC50 = 440.0 nM 6.36
CHEMBL4849845 — IC50 = 470.0 nM 6.33
CHEMBL4852597 — IC50 = 470.0 nM 6.33
CHEMBL4873869 — IC50 = 550.0 nM 6.26
CHEMBL4865127 — IC50 = 560.0 nM 6.25
CHEMBL4846549 — IC50 = 640.0 nM 6.19
CHEMBL4873354 — IC50 = 650.0 nM 6.19
CHEMBL4851109 — IC50 = 680.0 nM 6.17
CHEMBL4872706 — IC50 = 780.0 nM 6.11
CHEMBL4879217 — IC50 = 800.0 nM 6.10
CHEMBL4846454 — IC50 = 860.0 nM 6.07
CHEMBL4875424 — IC50 = 870.0 nM 6.06
CHEMBL4852248 — IC50 = 1000.0 nM 6.00
CHEMBL4853995 — IC50 = 1840.0 nM 5.74
CHEMBL4862528 — IC50 = 1880.0 nM 5.73
CHEMBL4878773 — IC50 = 2270.0 nM 5.64
CHEMBL4876958 — IC50 = 2880.0 nM 5.54
CHEMBL4866911 — IC50 = 5470.0 nM 5.26