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Assay Detail

CHEMBL3369904

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Functional
Antimalarial activity against multi-drug-resistant Plasmodium falciparum W2 infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay
ChEMBL ↗
61
Total Activities
61
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

Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
Cross RM, Flanigan DL, Monastyrskyi A, LaCrue AN, Sáenz FE, Maignan JR, Mutka TS, White KL, Shackleford DM, Bathurst I, Fronczek FR, Wojtas L, Guida WC, Charman SA, Burrows JN, Kyle DE, Manetsch R.
J Med Chem (2014) 57 : 8860 -8879
PubMed 25148516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 61 7.29 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3361389 — — 1 9.51
CHEMBL3361394 — — 1 9.22
CHEMBL3361395 — — 1 9.16
CHEMBL3361375 — — 1 8.89
CHEMBL1450 ATOVAQUONE 4.0 1 8.85
CHEMBL3361372 — — 1 8.75
CHEMBL3361388 — — 1 8.70
CHEMBL3361373 — — 1 8.62
CHEMBL3361390 — — 1 8.43
CHEMBL3361392 — — 1 8.29
CHEMBL307261 ARTENIMOL 3.0 1 8.26
CHEMBL3360786 — — 1 8.23
CHEMBL3361379 — — 1 8.20
CHEMBL3360791 — — 1 8.18
CHEMBL3361386 — — 1 8.12
CHEMBL3361391 — — 1 8.11
CHEMBL3361385 — — 1 8.11
CHEMBL3360788 — — 1 8.04
CHEMBL3361374 — — 1 7.97
CHEMBL3361353 — — 1 7.88
CHEMBL3361387 — — 1 7.85
CHEMBL3361376 — — 1 7.68
CHEMBL3361381 — — 1 7.67
CHEMBL3361365 — — 1 7.65
CHEMBL3360787 — — 1 7.61
CHEMBL3361377 — — 1 7.58
CHEMBL1257903 — — 1 7.58
CHEMBL3361352 — — 1 7.47
CHEMBL3361378 — — 1 7.45
CHEMBL3360789 — — 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3361389 — EC50 = 0.312 nM 9.51
CHEMBL3361394 — EC50 = 0.602 nM 9.22
CHEMBL3361395 — EC50 = 0.686 nM 9.16
CHEMBL3361375 — EC50 = 1.3 nM 8.89
CHEMBL1450 ATOVAQUONE EC50 = 1.4 nM 8.85
CHEMBL3361372 — EC50 = 1.78 nM 8.75
CHEMBL3361388 — EC50 = 2.02 nM 8.70
CHEMBL3361373 — EC50 = 2.4 nM 8.62
CHEMBL3361390 — EC50 = 3.74 nM 8.43
CHEMBL3361392 — EC50 = 5.18 nM 8.29
CHEMBL307261 ARTENIMOL EC50 = 5.5 nM 8.26
CHEMBL3360786 — EC50 = 5.83 nM 8.23
CHEMBL3361379 — EC50 = 6.25 nM 8.20
CHEMBL3360791 — EC50 = 6.65 nM 8.18
CHEMBL3361386 — EC50 = 7.52 nM 8.12
CHEMBL3361391 — EC50 = 7.74 nM 8.11
CHEMBL3361385 — EC50 = 7.72 nM 8.11
CHEMBL3360788 — EC50 = 9.15 nM 8.04
CHEMBL3361374 — EC50 = 10.6 nM 7.97
CHEMBL3361353 — EC50 = 13.3 nM 7.88
CHEMBL3361387 — EC50 = 14.2 nM 7.85
CHEMBL3361376 — EC50 = 20.8 nM 7.68
CHEMBL3361381 — EC50 = 21.4 nM 7.67
CHEMBL3361365 — EC50 = 22.5 nM 7.65
CHEMBL3360787 — EC50 = 24.5 nM 7.61
CHEMBL3361377 — EC50 = 26.3 nM 7.58
CHEMBL1257903 — EC50 = 26.2 nM 7.58
CHEMBL3361352 — EC50 = 34.2 nM 7.47
CHEMBL3361378 — EC50 = 35.7 nM 7.45
CHEMBL3360789 — EC50 = 46.0 nM 7.34
CHEMBL3361359 — EC50 = 49.0 nM 7.31
CHEMBL3361360 — EC50 = 54.0 nM 7.27
CHEMBL3361361 — EC50 = 58.4 nM 7.23
CHEMBL3361366 — EC50 = 60.7 nM 7.22
CHEMBL3360790 — EC50 = 61.7 nM 7.21
CHEMBL3360792 — EC50 = 66.8 nM 7.17
CHEMBL3361357 — EC50 = 71.8 nM 7.14
CHEMBL3361393 — EC50 = 73.4 nM 7.13
CHEMBL3360795 — EC50 = 128.0 nM 6.89
CHEMBL3361356 — EC50 = 133.0 nM 6.88
CHEMBL3361371 — EC50 = 154.0 nM 6.81
CHEMBL3361383 — EC50 = 157.0 nM 6.80
CHEMBL3361358 — EC50 = 173.0 nM 6.76
CHEMBL3361382 — EC50 = 194.0 nM 6.71
CHEMBL3361369 — EC50 = 258.0 nM 6.59
CHEMBL76 CHLOROQUINE EC50 = 421.0 nM 6.38
CHEMBL3361384 — EC50 = 443.0 nM 6.35
CHEMBL3361364 — EC50 = 517.0 nM 6.29
CHEMBL3361350 — EC50 = 748.0 nM 6.13
CHEMBL3360794 — EC50 = 748.0 nM 6.13