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Assay Detail

CHEMBL4388643

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Binding
Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured pig heart mitochondrial MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by spectrometric analysis
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GroEL/GroES (CHEMBL4106139)
Type PROTEIN COMPLEX
Organism Escherichia coli

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 72 4.49 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3986320 1 6.64
CHEMBL3938421 1 6.01
CHEMBL4176281 1 5.89
CHEMBL3913878 1 5.48
CHEMBL3903813 1 5.40
CHEMBL4463085 1 5.40
CHEMBL4168415 1 5.34
CHEMBL3975456 1 5.26
CHEMBL4437169 1 5.25
CHEMBL3910488 1 5.11
CHEMBL4168023 1 5.03
CHEMBL4573394 1 4.85
CHEMBL4556062 1 4.80
CHEMBL3922861 1 4.70
CHEMBL4449221 1 4.70
CHEMBL4561738 1 4.64
CHEMBL4461900 1 4.47
CHEMBL3906378 1 4.46
CHEMBL4563828 1 4.37
CHEMBL4434992 1 4.32
CHEMBL4461747 1 4.28
CHEMBL4567343 1 4.28
CHEMBL4458229 1 4.27
CHEMBL4458221 1 4.24
CHEMBL4567660 1 4.23
CHEMBL4558646 1 4.20
CHEMBL4464897 1 4.19
CHEMBL4448007 1 4.19
CHEMBL4570232 1 4.16
CHEMBL4567422 1 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3986320 IC50 = 230.0 nM 6.64
CHEMBL3938421 IC50 = 970.0 nM 6.01
CHEMBL4176281 IC50 = 1300.0 nM 5.89
CHEMBL3913878 IC50 = 3300.0 nM 5.48
CHEMBL3903813 IC50 = 4000.0 nM 5.40
CHEMBL4463085 IC50 = 4000.0 nM 5.40
CHEMBL4168415 IC50 = 4600.0 nM 5.34
CHEMBL3975456 IC50 = 5500.0 nM 5.26
CHEMBL4437169 IC50 = 5600.0 nM 5.25
CHEMBL3910488 IC50 = 7700.0 nM 5.11
CHEMBL4168023 IC50 = 9300.0 nM 5.03
CHEMBL4573394 IC50 = 14000.0 nM 4.85
CHEMBL4556062 IC50 = 16000.0 nM 4.80
CHEMBL4449221 IC50 = 20000.0 nM 4.70
CHEMBL3922861 IC50 = 20000.0 nM 4.70
CHEMBL4561738 IC50 = 23000.0 nM 4.64
CHEMBL4461900 IC50 = 34000.0 nM 4.47
CHEMBL3906378 IC50 = 35000.0 nM 4.46
CHEMBL4563828 IC50 = 43000.0 nM 4.37
CHEMBL4434992 IC50 = 48000.0 nM 4.32
CHEMBL4461747 IC50 = 53000.0 nM 4.28
CHEMBL4567343 IC50 = 53000.0 nM 4.28
CHEMBL4458229 IC50 = 54000.0 nM 4.27
CHEMBL4458221 IC50 = 58000.0 nM 4.24
CHEMBL4567660 IC50 = 59000.0 nM 4.23
CHEMBL4558646 IC50 = 63000.0 nM 4.20
CHEMBL4448007 IC50 = 64000.0 nM 4.19
CHEMBL4464897 IC50 = 64000.0 nM 4.19
CHEMBL4570232 IC50 = 70000.0 nM 4.16
CHEMBL4567422 IC50 = 72000.0 nM 4.14
CHEMBL4447680 IC50 = 76000.0 nM 4.12
CHEMBL4434972 IC50 = 76000.0 nM 4.12
CHEMBL4462640 IC50 = 75000.0 nM 4.12
CHEMBL4440273 IC50 = 78000.0 nM 4.11
CHEMBL4583096 IC50 = 77000.0 nM 4.11
CHEMBL4513591 IC50 = 79000.0 nM 4.10
CHEMBL4565368 IC50 = 79000.0 nM 4.10
CHEMBL4548800 IC50 = 81000.0 nM 4.09
CHEMBL4469657 IC50 = 83000.0 nM 4.08
CHEMBL4446756 IC50 = 86000.0 nM 4.07
CHEMBL4457015 IC50 = 85000.0 nM 4.07
CHEMBL4559209 IC50 = 90000.0 nM 4.05
CHEMBL4549691 IC50 = 90000.0 nM 4.05
CHEMBL4565061 IC50 = 92000.0 nM 4.04
CHEMBL4471032 IC50 = 92000.0 nM 4.04
CHEMBL4572554 IC50 = 92000.0 nM 4.04
CHEMBL4456802 IC50 = 91000.0 nM 4.04
CHEMBL4454247 IC50 = 92000.0 nM 4.04
CHEMBL4532359 IC50 = 91000.0 nM 4.04
CHEMBL4562717 IC50 = 93000.0 nM 4.03