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Assay Detail

CHEMBL2393744

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

Functional
Antimalarial activity against chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 infected in human red blood cells assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay
17
Total Activities
17
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

Synthesis and antimalarial testing of neocryptolepine analogues: addition of ester function in SAR study of 2,11-disubstituted indolo[2,3-b]quinolines.
Lu WJ, Wicht KJ, Wang L, Imai K, Mei ZW, Kaiser M, El Sayed Iel T, Egan TJ, Inokuchi T.
Eur J Med Chem (2013) 64 : 498 -511
PubMed 23685569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.41 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391247 1 7.92
CHEMBL2391089 1 7.80
CHEMBL2391095 1 7.79
CHEMBL2391087 1 7.78
CHEMBL2391090 1 7.72
CHEMBL2391086 1 7.71
CHEMBL2391248 1 7.70
CHEMBL2391246 1 7.66
CHEMBL2391242 1 7.63
CHEMBL2391249 1 7.52
CHEMBL2391240 1 7.39
CHEMBL2391241 1 7.30
CHEMBL2391094 1 7.25
CHEMBL2391097 1 7.19
CHEMBL2391096 1 7.17
CHEMBL76 CHLOROQUINE 4.0 1 6.68
CHEMBL115585 NEOCRYPTOLEPINE 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391247 IC50 = 11.9 nM 7.92
CHEMBL2391089 IC50 = 15.9 nM 7.80
CHEMBL2391095 IC50 = 16.1 nM 7.79
CHEMBL2391087 IC50 = 16.8 nM 7.78
CHEMBL2391090 IC50 = 19.2 nM 7.72
CHEMBL2391086 IC50 = 19.7 nM 7.71
CHEMBL2391248 IC50 = 20.2 nM 7.70
CHEMBL2391246 IC50 = 22.1 nM 7.66
CHEMBL2391242 IC50 = 23.3 nM 7.63
CHEMBL2391249 IC50 = 30.3 nM 7.52
CHEMBL2391240 IC50 = 40.8 nM 7.39
CHEMBL2391241 IC50 = 50.4 nM 7.30
CHEMBL2391094 IC50 = 56.1 nM 7.25
CHEMBL2391097 IC50 = 64.4 nM 7.19
CHEMBL2391096 IC50 = 68.4 nM 7.17
CHEMBL76 CHLOROQUINE IC50 = 210.0 nM 6.68
CHEMBL115585 NEOCRYPTOLEPINE IC50 = 1696.0 nM 5.77