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Assay Detail

CHEMBL1119992

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

Functional
Antimalarial activity against drug-sensitive Plasmodium falciparum NF54 infected in human erythrocytes after 48 hrs by [3H]hypoxanthine assay
21
Total Activities
21
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

Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.
Yeung BK, Zou B, Rottmann M, Lakshminarayana SB, Ang SH, Leong SY, Tan J, Wong J, Keller-Maerki S, Fischli C, Goh A, Schmitt EK, Krastel P, Francotte E, Kuhen K, Plouffe D, Henson K, Wagner T, Winzeler EA, Petersen F, Brun R, Dartois V, Diagana TT, Keller TH.
J Med Chem (2010) 53 : 5155 -5164
PubMed 20568778 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.40 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082725 1 9.70
CHEMBL1082723 CIPARGAMIN 2.0 1 9.05
CHEMBL1084349 1 8.52
CHEMBL1086475 1 8.40
CHEMBL1083769 1 8.05
CHEMBL1083766 1 7.70
CHEMBL1083768 1 7.57
CHEMBL1082724 1 7.11
CHEMBL1086478 1 7.08
CHEMBL1083770 1 7.08
CHEMBL1085620 1 7.07
CHEMBL1085114 SPIROAZEPINEINDOLE 1 7.05
CHEMBL1084948 1 6.94
CHEMBL1084077 1 6.90
CHEMBL1083219 1 6.74
CHEMBL1085371 1 6.35
CHEMBL1084078 1 6.07
CHEMBL1085370 1 5.74
CHEMBL1083767 1 -
CHEMBL1084073 1 -
CHEMBL1085369 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082725 IC50 = 0.2 nM 9.70
CHEMBL1082723 CIPARGAMIN IC50 = 0.9 nM 9.05
CHEMBL1084349 IC50 = 3.0 nM 8.52
CHEMBL1086475 IC50 = 4.0 nM 8.40
CHEMBL1083769 IC50 = 9.0 nM 8.05
CHEMBL1083766 IC50 = 20.0 nM 7.70
CHEMBL1083768 IC50 = 27.0 nM 7.57
CHEMBL1082724 IC50 = 77.0 nM 7.11
CHEMBL1086478 IC50 = 83.0 nM 7.08
CHEMBL1083770 IC50 = 84.0 nM 7.08
CHEMBL1085620 IC50 = 86.0 nM 7.07
CHEMBL1085114 SPIROAZEPINEINDOLE IC50 = 90.0 nM 7.05
CHEMBL1084948 IC50 = 116.0 nM 6.94
CHEMBL1084077 IC50 = 126.0 nM 6.90
CHEMBL1083219 IC50 = 182.0 nM 6.74
CHEMBL1085371 IC50 = 444.0 nM 6.35
CHEMBL1084078 IC50 = 857.0 nM 6.07
CHEMBL1085370 IC50 = 1808.0 nM 5.74
CHEMBL1083767 IC50 > 5000.0 nM -
CHEMBL1084073 IC50 > 5000.0 nM -
CHEMBL1085369 IC50 > 5000.0 nM -