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Assay Detail

CHEMBL5381256

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Functional
Antitrypanosomal activity against Trypanosoma brucei Lister 427 assessed as parasite growth inhibition incubated for 1 hr under dark condition by fluorometer analysis
ChEMBL ↗
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei (CHEMBL612849) ↗
Type ORGANISM
Organism Trypanosoma brucei

Publication

Chemical Optimization of CBL0137 for Human African Trypanosomiasis Lead Drug Discovery.
Singh B, Sharma A, Gunaganti N, Rivers M, Gadekar PK, Greene B, Chichioco M, Sanz-Rodriguez CE, Fu C, LeBlanc C, Burchfield E, Sharif N, Hoffman B, Kumar G, Purmal A, Mensa-Wilmot K, Pollastri MP.
J Med Chem (2023) 66 : 1972 -1989
PubMed 36695630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 63 6.70 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397299 — — 1 8.10
CHEMBL5434172 — — 1 7.68
CHEMBL5422179 — — 1 7.62
CHEMBL5411703 — — 1 7.60
CHEMBL5433187 — — 1 7.54
CHEMBL5427644 — — 1 7.52
CHEMBL5429852 — — 1 7.52
CHEMBL5403943 — — 1 7.50
CHEMBL5434709 — — 1 7.50
CHEMBL5396971 — — 1 7.46
CHEMBL4640631 — — 1 7.43
CHEMBL5418105 — — 1 7.34
CHEMBL5426473 — — 1 7.34
CHEMBL5424663 — — 1 7.32
CHEMBL5422939 — — 1 7.31
CHEMBL5419521 — — 1 7.28
CHEMBL5422754 — — 1 7.24
CHEMBL5428312 — — 1 7.13
CHEMBL5418263 — — 1 7.08
CHEMBL5412675 — — 1 7.00
CHEMBL5416404 — — 1 6.96
CHEMBL5402782 — — 1 6.96
CHEMBL5429064 — — 1 6.92
CHEMBL5439254 — — 1 6.89
CHEMBL5419408 — — 1 6.89
CHEMBL5394429 — — 1 6.89
CHEMBL5437860 — — 1 6.77
CHEMBL5436145 — — 1 6.75
CHEMBL5431376 — — 1 6.75
CHEMBL5405942 — — 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397299 — EC50 = 8.0 nM 8.10
CHEMBL5434172 — EC50 = 21.0 nM 7.68
CHEMBL5422179 — EC50 = 24.0 nM 7.62
CHEMBL5411703 — EC50 = 25.0 nM 7.60
CHEMBL5433187 — EC50 = 29.0 nM 7.54
CHEMBL5427644 — EC50 = 30.0 nM 7.52
CHEMBL5429852 — EC50 = 30.0 nM 7.52
CHEMBL5403943 — EC50 = 32.0 nM 7.50
CHEMBL5434709 — EC50 = 32.0 nM 7.50
CHEMBL5396971 — EC50 = 35.0 nM 7.46
CHEMBL4640631 — EC50 = 37.0 nM 7.43
CHEMBL5418105 — EC50 = 46.0 nM 7.34
CHEMBL5426473 — EC50 = 46.0 nM 7.34
CHEMBL5424663 — EC50 = 48.0 nM 7.32
CHEMBL5422939 — EC50 = 49.0 nM 7.31
CHEMBL5419521 — EC50 = 52.0 nM 7.28
CHEMBL5422754 — EC50 = 57.0 nM 7.24
CHEMBL5428312 — EC50 = 74.0 nM 7.13
CHEMBL5418263 — EC50 = 84.0 nM 7.08
CHEMBL5412675 — EC50 = 100.0 nM 7.00
CHEMBL5416404 — EC50 = 110.0 nM 6.96
CHEMBL5402782 — EC50 = 110.0 nM 6.96
CHEMBL5429064 — EC50 = 120.0 nM 6.92
CHEMBL5394429 — EC50 = 130.0 nM 6.89
CHEMBL5439254 — EC50 = 130.0 nM 6.89
CHEMBL5419408 — EC50 = 130.0 nM 6.89
CHEMBL5437860 — EC50 = 170.0 nM 6.77
CHEMBL5436145 — EC50 = 180.0 nM 6.75
CHEMBL5431376 — EC50 = 180.0 nM 6.75
CHEMBL5405942 — EC50 = 190.0 nM 6.72
CHEMBL5438742 — EC50 = 230.0 nM 6.64
CHEMBL5419149 — EC50 = 230.0 nM 6.64
CHEMBL5408980 — EC50 = 260.0 nM 6.58
CHEMBL5403737 — EC50 = 270.0 nM 6.57
CHEMBL5432150 — EC50 = 280.0 nM 6.55
CHEMBL5431386 — EC50 = 340.0 nM 6.47
CHEMBL5408928 — EC50 = 350.0 nM 6.46
CHEMBL5400368 — EC50 = 350.0 nM 6.46
CHEMBL5437175 — EC50 = 400.0 nM 6.40
CHEMBL5435529 — EC50 = 410.0 nM 6.39
CHEMBL5426414 — EC50 = 420.0 nM 6.38
CHEMBL5431979 — EC50 = 430.0 nM 6.37
CHEMBL5422178 — EC50 = 450.0 nM 6.35
CHEMBL5413889 — EC50 = 490.0 nM 6.31
CHEMBL5435983 — EC50 = 570.0 nM 6.24
CHEMBL5415135 — EC50 = 620.0 nM 6.21
CHEMBL5424432 — EC50 = 650.0 nM 6.19
CHEMBL5406923 — EC50 = 810.0 nM 6.09
CHEMBL5396180 — EC50 = 1100.0 nM 5.96
CHEMBL5414318 — EC50 = 1100.0 nM 5.96