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Assay Detail

CHEMBL4388634

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Binding
Inhibition of Mycobacterium tuberculosis His-tagged PtpB expressed in Escherichia coli Rosetta 2 (DE3) using pNPP as substrate after 30 mins by spectrophotometric method
146
Total Activities
146
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phosphotyrosine protein phosphatase (CHEMBL4295521)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections.
Washburn A, Abdeen S, Ovechkina Y, Ray AM, Stevens M, Chitre S, Sivinski J, Park Y, Johnson J, Hoang QQ, Chapman E, Parish T, Johnson SM.
Bioorg Med Chem Lett (2019) 29 : 1665 -1672
PubMed 31047750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 146 4.82 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3942054 1 6.10
CHEMBL3938421 1 5.82
CHEMBL4161487 1 5.70
CHEMBL3934460 1 5.68
CHEMBL4453551 1 5.66
CHEMBL3904891 1 5.64
CHEMBL3910488 1 5.64
CHEMBL4162794 1 5.64
CHEMBL4542408 1 5.64
CHEMBL4590591 1 5.57
CHEMBL3908434 1 5.55
CHEMBL3970551 1 5.54
CHEMBL4160098 1 5.52
CHEMBL4166077 1 5.48
CHEMBL4447455 1 5.47
CHEMBL4446055 1 5.47
CHEMBL3979736 1 5.44
CHEMBL4545651 1 5.44
CHEMBL4169499 1 5.42
CHEMBL4518473 1 5.41
CHEMBL4533148 1 5.41
CHEMBL4167333 1 5.40
CHEMBL4548710 1 5.39
CHEMBL4449994 1 5.39
CHEMBL3924343 1 5.38
CHEMBL3975683 1 5.37
CHEMBL4171392 1 5.36
CHEMBL4168415 1 5.36
CHEMBL4161583 1 5.34
CHEMBL3950773 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3942054 IC50 = 790.0 nM 6.10
CHEMBL3938421 IC50 = 1500.0 nM 5.82
CHEMBL4161487 IC50 = 2000.0 nM 5.70
CHEMBL3934460 IC50 = 2100.0 nM 5.68
CHEMBL4453551 IC50 = 2200.0 nM 5.66
CHEMBL3904891 IC50 = 2300.0 nM 5.64
CHEMBL4542408 IC50 = 2300.0 nM 5.64
CHEMBL4162794 IC50 = 2300.0 nM 5.64
CHEMBL3910488 IC50 = 2300.0 nM 5.64
CHEMBL4590591 IC50 = 2700.0 nM 5.57
CHEMBL3908434 IC50 = 2800.0 nM 5.55
CHEMBL3970551 IC50 = 2900.0 nM 5.54
CHEMBL4160098 IC50 = 3000.0 nM 5.52
CHEMBL4166077 IC50 = 3300.0 nM 5.48
CHEMBL4447455 IC50 = 3400.0 nM 5.47
CHEMBL4446055 IC50 = 3400.0 nM 5.47
CHEMBL3979736 IC50 = 3600.0 nM 5.44
CHEMBL4545651 IC50 = 3600.0 nM 5.44
CHEMBL4169499 IC50 = 3800.0 nM 5.42
CHEMBL4518473 IC50 = 3900.0 nM 5.41
CHEMBL4533148 IC50 = 3900.0 nM 5.41
CHEMBL4167333 IC50 = 4000.0 nM 5.40
CHEMBL4548710 IC50 = 4100.0 nM 5.39
CHEMBL4449994 IC50 = 4100.0 nM 5.39
CHEMBL3924343 IC50 = 4200.0 nM 5.38
CHEMBL3975683 IC50 = 4300.0 nM 5.37
CHEMBL4168415 IC50 = 4400.0 nM 5.36
CHEMBL4171392 IC50 = 4400.0 nM 5.36
CHEMBL4161583 IC50 = 4600.0 nM 5.34
CHEMBL3950773 IC50 = 4900.0 nM 5.31
CHEMBL4562570 IC50 = 5000.0 nM 5.30
CHEMBL4463085 IC50 = 5100.0 nM 5.29
CHEMBL4513892 IC50 = 5300.0 nM 5.28
CHEMBL4531689 IC50 = 5400.0 nM 5.27
CHEMBL4467368 IC50 = 5500.0 nM 5.26
CHEMBL3933283 IC50 = 5800.0 nM 5.24
CHEMBL4531228 IC50 = 5700.0 nM 5.24
CHEMBL3890411 IC50 = 5800.0 nM 5.24
CHEMBL4168023 IC50 = 5900.0 nM 5.23
CHEMBL3955935 IC50 = 6200.0 nM 5.21
CHEMBL4526007 IC50 = 6400.0 nM 5.19
CHEMBL3983712 IC50 = 6400.0 nM 5.19
CHEMBL4449196 IC50 = 6500.0 nM 5.19
CHEMBL3980253 IC50 = 6400.0 nM 5.19
CHEMBL4547546 IC50 = 6800.0 nM 5.17
CHEMBL4521813 IC50 = 6700.0 nM 5.17
CHEMBL3912547 IC50 = 7000.0 nM 5.16
CHEMBL1389174 IC50 = 6900.0 nM 5.16
CHEMBL4176697 IC50 = 7100.0 nM 5.15
CHEMBL4565697 IC50 = 7100.0 nM 5.15