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Assay Detail

CHEMBL4481394

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Functional
Antimicrobial activity against Wolbachia wMel infected in Drosophila melanogaster LDW1 cells after 6 days by DAPI-based fluorescence in-situ hybridization assay
ChEMBL ↗
72
Total Activities
72
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Wolbachia
Confidence 1 — Organism
Curated By Autocuration

Target

Wolbachia (CHEMBL4630676) ↗
Type ORGANISM
Organism Wolbachia

Publication

Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
Jacobs RT, Lunde CS, Freund YR, Hernandez V, Li X, Xia Y, Carter DS, Berry PW, Halladay J, Rock F, Stefanakis R, Easom E, Plattner JJ, Ford L, Johnston KL, Cook DAN, Clare R, Cassidy A, Myhill L, Tyrer H, Gamble J, Guimaraes AF, Steven A, Lenz F, Ehrens A, Frohberger SJ, Koschel M, Hoerauf A, Hübner MP, McNamara CW, Bakowski MA, Turner JD, Taylor MJ, Ward SA.
J Med Chem (2019) 62 : 2521 -2540
PubMed 30730745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 71 7.59 9.70
IC50 1 6.71 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4566922 — — 1 9.70
CHEMBL4483699 — — 1 9.70
CHEMBL4542784 — — 1 9.52
CHEMBL4578840 — — 1 9.10
CHEMBL4551406 — — 1 8.92
CHEMBL4533414 — — 1 8.89
CHEMBL4532724 — — 1 8.89
CHEMBL4552978 — — 1 8.82
CHEMBL4535824 — — 1 8.82
CHEMBL4557144 — — 1 8.57
CHEMBL4525311 — — 1 8.57
CHEMBL4551336 — — 1 8.55
CHEMBL4539733 — — 1 8.54
CHEMBL4522659 — — 1 8.46
CHEMBL4575078 — — 1 8.43
CHEMBL4589897 — — 1 8.39
CHEMBL4529660 — — 1 8.31
CHEMBL4575394 — — 1 8.29
CHEMBL1688852 VALNEMULIN 2.0 1 8.21
CHEMBL4576782 — — 1 8.20
CHEMBL4535683 — — 1 8.12
CHEMBL4592079 — — 1 8.05
CHEMBL4540795 — — 1 7.96
CHEMBL4547028 — — 1 7.89
CHEMBL4552098 — — 1 7.89
CHEMBL4553678 — — 1 7.85
CHEMBL4569244 — — 1 7.85
CHEMBL4570403 — — 1 7.82
CHEMBL4587910 — — 1 7.77
CHEMBL4592244 — — 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4566922 — EC50 = 0.2 nM 9.70
CHEMBL4483699 — EC50 = 0.2 nM 9.70
CHEMBL4542784 — EC50 = 0.3 nM 9.52
CHEMBL4578840 — EC50 = 0.8 nM 9.10
CHEMBL4551406 — EC50 = 1.2 nM 8.92
CHEMBL4533414 — EC50 = 1.3 nM 8.89
CHEMBL4532724 — EC50 = 1.3 nM 8.89
CHEMBL4552978 — EC50 = 1.5 nM 8.82
CHEMBL4535824 — EC50 = 1.5 nM 8.82
CHEMBL4557144 — EC50 = 2.7 nM 8.57
CHEMBL4525311 — EC50 = 2.7 nM 8.57
CHEMBL4551336 — EC50 = 2.8 nM 8.55
CHEMBL4539733 — EC50 = 2.9 nM 8.54
CHEMBL4522659 — EC50 = 3.5 nM 8.46
CHEMBL4575078 — EC50 = 3.7 nM 8.43
CHEMBL4589897 — EC50 = 4.1 nM 8.39
CHEMBL4529660 — EC50 = 4.9 nM 8.31
CHEMBL4575394 — EC50 = 5.1 nM 8.29
CHEMBL1688852 VALNEMULIN EC50 = 6.1 nM 8.21
CHEMBL4576782 — EC50 = 6.3 nM 8.20
CHEMBL4535683 — EC50 = 7.5 nM 8.12
CHEMBL4592079 — EC50 = 9.0 nM 8.05
CHEMBL4540795 — EC50 = 11.0 nM 7.96
CHEMBL4547028 — EC50 = 13.0 nM 7.89
CHEMBL4552098 — EC50 = 13.0 nM 7.89
CHEMBL4553678 — EC50 = 14.0 nM 7.85
CHEMBL4569244 — EC50 = 14.0 nM 7.85
CHEMBL4570403 — EC50 = 15.0 nM 7.82
CHEMBL4587910 — EC50 = 17.0 nM 7.77
CHEMBL4592244 — EC50 = 17.0 nM 7.77
CHEMBL4519273 — EC50 = 18.0 nM 7.75
CHEMBL4527402 — EC50 = 19.0 nM 7.72
CHEMBL4518696 — EC50 = 19.0 nM 7.72
CHEMBL4576039 — EC50 = 24.0 nM 7.62
CHEMBL4546281 — EC50 = 27.0 nM 7.57
CHEMBL4565868 — EC50 = 28.0 nM 7.55
CHEMBL4526326 — EC50 = 29.0 nM 7.54
CHEMBL4520153 — EC50 = 33.0 nM 7.48
CHEMBL4527454 — EC50 = 39.0 nM 7.41
CHEMBL4559425 — EC50 = 39.0 nM 7.41
CHEMBL4544063 — EC50 = 44.0 nM 7.36
CHEMBL4521532 — EC50 = 44.0 nM 7.36
CHEMBL4548875 — EC50 = 49.0 nM 7.31
CHEMBL4592238 — EC50 = 71.0 nM 7.15
CHEMBL1658 RETAPAMULIN EC50 = 91.0 nM 7.04
CHEMBL4581396 — EC50 = 101.0 nM 7.00
CHEMBL4544226 — EC50 = 133.0 nM 6.88
CHEMBL4556110 — EC50 = 148.0 nM 6.83
CHEMBL4515909 — EC50 = 173.0 nM 6.76
CHEMBL4542505 — IC50 = 193.0 nM 6.71