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Assay Detail

CHEMBL1789906

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Functional
NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration
ChEMBL ↗
678
Total Activities
338
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium yoelii
Cell Type HepG2-A16-CD81
Confidence 1 — Organism
Curated By Expert

Target

Plasmodium yoelii (CHEMBL612889) ↗
Type ORGANISM
Organism Plasmodium yoelii

Publication

Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Meister S, Plouffe DM, Kuhen KL, Bonamy GM, Wu T, Barnes SW, Bopp SE, Borboa R, Bright AT, Che J, Cohen S, Dharia NV, Gagaring K, Gettayacamin M, Gordon P, Groessl T, Kato N, Lee MC, McNamara CW, Fidock DA, Nagle A, Nam TG, Richmond W, Roland J, Rottmann M, Zhou B, Froissard P, Glynne RJ, Mazier D, Sattabongkot J, Schultz PG, Tuntland T, Walker JR, Zhou Y, Chatterjee A, Diagana TT, Winzeler EA.
Science (2011) 334 : 1372 -1377
PubMed 22096101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 339 6.68 8.73
Schizont size 339 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL578967 — — 2 8.73
CHEMBL36 PYRIMETHAMINE 4.0 2 8.67
CHEMBL600754 — — 2 8.64
CHEMBL544227 CHLORCYCLOGUANIL HYDROCHLORIDE — 2 8.59
CHEMBL581449 — — 2 8.38
CHEMBL602181 — — 2 8.37
CHEMBL586955 — — 2 8.35
CHEMBL533376 — — 2 8.31
CHEMBL602193 — — 2 8.21
CHEMBL600766 — — 2 8.17
CHEMBL598053 — — 2 8.15
CHEMBL50588 EMETINE 4.0 2 8.13
CHEMBL535267 — — 2 8.00
CHEMBL548155 — — 2 8.00
CHEMBL602174 — — 2 7.97
CHEMBL602612 — — 2 7.97
CHEMBL580848 — — 2 7.96
CHEMBL602562 — — 2 7.95
CHEMBL602978 — — 2 7.95
CHEMBL587259 — — 2 7.95
CHEMBL582456 — — 2 7.94
CHEMBL611663 — — 2 7.88
CHEMBL578681 — — 2 7.87
CHEMBL1186409 — — 2 7.85
CHEMBL600753 — — 2 7.84
CHEMBL602164 — — 2 7.82
CHEMBL576810 — — 2 7.76
CHEMBL579352 — — 2 7.76
CHEMBL600295 — — 2 7.73
CHEMBL601766 — — 2 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL578967 — IC50 = 1.85 nM 8.73
CHEMBL36 PYRIMETHAMINE IC50 = 2.152 nM 8.67
CHEMBL600754 — IC50 = 2.286 nM 8.64
CHEMBL544227 CHLORCYCLOGUANIL HYDROCHLORIDE IC50 = 2.56 nM 8.59
CHEMBL581449 — IC50 = 4.18 nM 8.38
CHEMBL602181 — IC50 = 4.25 nM 8.37
CHEMBL586955 — IC50 = 4.5 nM 8.35
CHEMBL533376 — IC50 = 4.93 nM 8.31
CHEMBL602193 — IC50 = 6.21 nM 8.21
CHEMBL600766 — IC50 = 6.76 nM 8.17
CHEMBL598053 — IC50 = 7.13 nM 8.15
CHEMBL50588 EMETINE IC50 = 7.49 nM 8.13
CHEMBL535267 — IC50 = 10.0 nM 8.00
CHEMBL548155 — IC50 = 10.0 nM 8.00
CHEMBL602612 — IC50 = 10.71 nM 7.97
CHEMBL602174 — IC50 = 10.76 nM 7.97
CHEMBL580848 — IC50 = 10.88 nM 7.96
CHEMBL602562 — IC50 = 11.24 nM 7.95
CHEMBL602978 — IC50 = 11.27 nM 7.95
CHEMBL587259 — IC50 = 11.27 nM 7.95
CHEMBL582456 — IC50 = 11.52 nM 7.94
CHEMBL611663 — IC50 = 13.24 nM 7.88
CHEMBL578681 — IC50 = 13.56 nM 7.87
CHEMBL1186409 — IC50 = 14.03 nM 7.85
CHEMBL600753 — IC50 = 14.48 nM 7.84
CHEMBL602164 — IC50 = 15.05 nM 7.82
CHEMBL579352 — IC50 = 17.47 nM 7.76
CHEMBL576810 — IC50 = 17.38 nM 7.76
CHEMBL600295 — IC50 = 18.59 nM 7.73
CHEMBL601766 — IC50 = 18.92 nM 7.72
CHEMBL597855 — IC50 = 20.0 nM 7.70
CHEMBL601594 — IC50 = 20.21 nM 7.69
CHEMBL587902 — IC50 = 20.43 nM 7.69
CHEMBL582672 — IC50 = 22.31 nM 7.65
CHEMBL600521 — IC50 = 25.53 nM 7.59
CHEMBL602024 — IC50 = 25.61 nM 7.59
CHEMBL601598 — IC50 = 29.3 nM 7.53
CHEMBL598883 — IC50 = 29.48 nM 7.53
CHEMBL2368645 — IC50 = 33.5 nM 7.47
CHEMBL581868 — IC50 = 34.6 nM 7.46
CHEMBL600755 — IC50 = 38.1 nM 7.42
CHEMBL602371 — IC50 = 39.4 nM 7.41
CHEMBL530973 — IC50 = 42.1 nM 7.38
CHEMBL587611 — IC50 = 43.8 nM 7.36
CHEMBL578944 — IC50 = 45.5 nM 7.34
CHEMBL528492 — IC50 = 46.8 nM 7.33
CHEMBL577011 — IC50 = 47.3 nM 7.33
CHEMBL524376 — IC50 = 47.9 nM 7.32
CHEMBL580166 — IC50 = 47.4 nM 7.32
CHEMBL601113 — IC50 = 47.9 nM 7.32