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Assay Detail

CHEMBL3584880

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

Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 cultured in human erythrocytes assessed as inhibition of parasite growth incubated for 48 hrs by YOYO-1 staining based flow cytometry
34
Total Activities
34
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

Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.
Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Sanders V, Freund YR, Campo B, Rosenthal PJ, Bu W, Gamo FJ, Sanz LM, Ge M, Li L, Ding J, Yang Y.
J Med Chem (2015) 58 : 5344 -5354
PubMed 26067904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.37 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581500 1 9.70
CHEMBL3581502 1 9.40
CHEMBL3581499 1 9.30
CHEMBL3581497 1 9.30
CHEMBL3581503 1 9.15
CHEMBL3581498 1 8.92
CHEMBL3581479 1 8.85
CHEMBL269671 ARTEMISININ 3.0 1 8.22
CHEMBL3581504 1 8.18
CHEMBL3581501 1 7.72
CHEMBL76 CHLOROQUINE 4.0 1 7.68
CHEMBL3581476 1 7.64
CHEMBL3581478 1 7.09
CHEMBL3581483 1 6.96
CHEMBL3581487 1 6.92
CHEMBL1761274 1 6.92
CHEMBL3581488 1 6.82
CHEMBL1761275 1 6.82
CHEMBL3581475 1 6.77
CHEMBL3581505 1 6.72
CHEMBL3581491 1 6.72
CHEMBL3581485 1 6.68
CHEMBL3581486 1 6.62
CHEMBL3581482 1 6.36
CHEMBL3581481 1 6.33
CHEMBL3581494 1 6.10
CHEMBL3581492 1 5.75
CHEMBL3581490 1 5.18
CHEMBL3581480 1 5.03
CHEMBL3581493 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581500 IC50 = 0.2 nM 9.70
CHEMBL3581502 IC50 = 0.4 nM 9.40
CHEMBL3581499 IC50 = 0.5 nM 9.30
CHEMBL3581497 IC50 = 0.5 nM 9.30
CHEMBL3581503 IC50 = 0.7 nM 9.15
CHEMBL3581498 IC50 = 1.2 nM 8.92
CHEMBL3581479 IC50 = 1.4 nM 8.85
CHEMBL269671 ARTEMISININ IC50 = 6.0 nM 8.22
CHEMBL3581504 IC50 = 6.6 nM 8.18
CHEMBL3581501 IC50 = 19.0 nM 7.72
CHEMBL76 CHLOROQUINE IC50 = 21.0 nM 7.68
CHEMBL3581476 IC50 = 23.0 nM 7.64
CHEMBL3581478 IC50 = 82.0 nM 7.09
CHEMBL3581483 IC50 = 110.0 nM 6.96
CHEMBL1761274 IC50 = 120.0 nM 6.92
CHEMBL3581487 IC50 = 120.0 nM 6.92
CHEMBL1761275 IC50 = 150.0 nM 6.82
CHEMBL3581488 IC50 = 150.0 nM 6.82
CHEMBL3581475 IC50 = 170.0 nM 6.77
CHEMBL3581505 IC50 = 190.0 nM 6.72
CHEMBL3581491 IC50 = 190.0 nM 6.72
CHEMBL3581485 IC50 = 210.0 nM 6.68
CHEMBL3581486 IC50 = 240.0 nM 6.62
CHEMBL3581482 IC50 = 440.0 nM 6.36
CHEMBL3581481 IC50 = 470.0 nM 6.33
CHEMBL3581494 IC50 = 800.0 nM 6.10
CHEMBL3581492 IC50 = 1770.0 nM 5.75
CHEMBL3581490 IC50 = 6660.0 nM 5.18
CHEMBL3581480 IC50 = 9380.0 nM 5.03
CHEMBL3581493 IC50 > 10000.0 nM -
CHEMBL3581484 IC50 > 10000.0 nM -
CHEMBL3581495 IC50 > 10000.0 nM -
CHEMBL3581496 IC50 > 10000.0 nM -
CHEMBL3581489 IC50 > 10000.0 nM -