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Assay Detail

CHEMBL3820114

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

Binding
Inhibition of ATP synthase in Mycobacterium smegmatis inverted membrane vesicles assessed as reduction in oxidative phosphorylation of ADP incubated for 60 mins in presence of NADH by luciferin/luciferase coupled reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycolicibacterium smegmatis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Scaffold morphing leading to evolution of 2,4-diaminoquinolines and aminopyrazolopyrimidines as inhibitors of the ATP synthesis pathway
Tantry SJ, Shinde V, Balakrishnan G, Markad SD, Gupta AK, Bhat J, Narayan A, Raichurkar A, Jena LK, Sharma S, Kumar N, Nanduri R, Bharath S, Reddy J, Panduga V, Prabhakar KR, Kandaswamy K, Kaur P, Dinesh N, Guptha S, Saralaya R, Panda M, Rudrapatna S, Mallya M, Rubin H, Yano T, Mdluili K, Cooper CB, Balasubramanian V, Sambandamurthy VK, Ramachandran V, Shandil R, Kavanagh S, Narayanan S, Iyer P, Mukherjee K, Hosagrahara VP, Solapure S, Hameed P S, Ravishankar S
Medchemcomm (2016) 7 : 1022 -1032
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.38 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376488 BEDAQUILINE 4.0 1 8.30
CHEMBL3819336 1 7.40
CHEMBL3818021 1 7.22
CHEMBL3819273 1 7.22
CHEMBL3818461 1 7.00
CHEMBL3819419 1 7.00
CHEMBL3819455 1 7.00
CHEMBL3818001 1 7.00
CHEMBL3818964 1 7.00
CHEMBL3818425 1 7.00
CHEMBL3819381 1 6.40
CHEMBL3817907 1 6.35
CHEMBL3818181 1 6.30
CHEMBL3819212 1 6.22
CHEMBL3819568 1 6.10
CHEMBL3819365 1 6.05
CHEMBL3819462 1 5.77
CHEMBL1449930 1 5.68
CHEMBL1498173 1 5.60
CHEMBL3818431 1 5.43
CHEMBL224214 CARBONYL CYANIDE M-CHLOROPHENYLHYDRAZONE 1 5.32
CHEMBL3818865 1 4.68
CHEMBL3819498 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376488 BEDAQUILINE IC50 = 5.0 nM 8.30
CHEMBL3819336 IC50 = 40.0 nM 7.40
CHEMBL3818021 IC50 = 60.0 nM 7.22
CHEMBL3819273 IC50 = 60.0 nM 7.22
CHEMBL3818461 IC50 = 100.0 nM 7.00
CHEMBL3819419 IC50 = 100.0 nM 7.00
CHEMBL3819455 IC50 = 100.0 nM 7.00
CHEMBL3818001 IC50 = 100.0 nM 7.00
CHEMBL3818964 IC50 = 100.0 nM 7.00
CHEMBL3818425 IC50 = 100.0 nM 7.00
CHEMBL3819381 IC50 = 400.0 nM 6.40
CHEMBL3817907 IC50 = 450.0 nM 6.35
CHEMBL3818181 IC50 = 500.0 nM 6.30
CHEMBL3819212 IC50 = 600.0 nM 6.22
CHEMBL3819568 IC50 = 800.0 nM 6.10
CHEMBL3819365 IC50 = 900.0 nM 6.05
CHEMBL3819462 IC50 = 1700.0 nM 5.77
CHEMBL1449930 IC50 = 2100.0 nM 5.68
CHEMBL1498173 IC50 = 2500.0 nM 5.60
CHEMBL3818431 IC50 = 3700.0 nM 5.43
CHEMBL224214 CARBONYL CYANIDE M-CHLOROPHENYLHYDRAZONE IC50 = 4800.0 nM 5.32
CHEMBL3818865 IC50 = 21000.0 nM 4.68
CHEMBL3819498 IC50 = 25000.0 nM 4.60