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Assay Detail

CHEMBL4392934

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Binding
Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis
58
Total Activities
58
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

HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.
Stevens M, Abdeen S, Salim N, Ray AM, Washburn A, Chitre S, Sivinski J, Park Y, Hoang QQ, Chapman E, Johnson SM.
Bioorg Med Chem Lett (2019) 29 : 1106 -1112
PubMed 30852084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 5.24 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1200712 EVANS BLUE 4.0 1 7.06
CHEMBL295316 PLUMBAGIN 1.0 1 6.54
CHEMBL253570 GOSSYPETIN 1 6.41
CHEMBL1516388 1 6.37
CHEMBL704 MESALAMINE 4.0 1 6.31
CHEMBL275938 AURINTRICARBOXYLIC ACID 1 6.24
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 6.24
CHEMBL15192 LAPACHONE 2.0 1 6.23
CHEMBL3989697 RIBOFLAVIN 5'-PHOSPHATE SODIUM 4.0 1 6.11
CHEMBL506247 TANNIC ACID 4.0 1 6.00
CHEMBL1360563 HEMATEIN 1 5.92
CHEMBL5483017 1 5.92
CHEMBL4448756 1 5.70
CHEMBL12131 CLOSANTEL 2.0 1 5.70
CHEMBL284328 HOMIDIUM BROMIDE 2.0 1 5.62
CHEMBL590 MENADIONE 4.0 1 5.60
CHEMBL140 CURCUMIN 3.0 1 5.54
CHEMBL1325592 PROTOPORPHYRIN -1.0 1 5.52
CHEMBL550495 METHYLENE BLUE 4.0 1 5.48
CHEMBL294264 PURPURIN 1 5.40
CHEMBL496 HEXACHLOROPHENE 4.0 1 5.33
CHEMBL456 ETHACRYNIC ACID 4.0 1 5.33
CHEMBL1265 ADAPALENE 4.0 1 5.29
CHEMBL28626 MORIN 1 5.28
CHEMBL506 PRIMAQUINE 4.0 1 5.21
CHEMBL220190 ASCORBYL PALMITATE -1.0 1 5.07
CHEMBL78764 1 5.05
CHEMBL2003538 CETYLPYRIDINIUM CHLORIDE 3.0 1 5.05
CHEMBL5314343 1 4.92
CHEMBL290106 BITHIONOL 4.0 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1200712 EVANS BLUE IC50 = 87.0 nM 7.06
CHEMBL295316 PLUMBAGIN IC50 = 290.0 nM 6.54
CHEMBL253570 GOSSYPETIN IC50 = 390.0 nM 6.41
CHEMBL1516388 IC50 = 430.0 nM 6.37
CHEMBL704 MESALAMINE IC50 = 490.0 nM 6.31
CHEMBL275938 AURINTRICARBOXYLIC ACID IC50 = 570.0 nM 6.24
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 580.0 nM 6.24
CHEMBL15192 LAPACHONE IC50 = 590.0 nM 6.23
CHEMBL3989697 RIBOFLAVIN 5'-PHOSPHATE SODIUM IC50 = 770.0 nM 6.11
CHEMBL506247 TANNIC ACID IC50 = 1000.0 nM 6.00
CHEMBL1360563 HEMATEIN IC50 = 1200.0 nM 5.92
CHEMBL5483017 IC50 = 1200.0 nM 5.92
CHEMBL4448756 IC50 = 2000.0 nM 5.70
CHEMBL12131 CLOSANTEL IC50 = 2000.0 nM 5.70
CHEMBL284328 HOMIDIUM BROMIDE IC50 = 2400.0 nM 5.62
CHEMBL590 MENADIONE IC50 = 2500.0 nM 5.60
CHEMBL140 CURCUMIN IC50 = 2900.0 nM 5.54
CHEMBL1325592 PROTOPORPHYRIN IC50 = 3000.0 nM 5.52
CHEMBL550495 METHYLENE BLUE IC50 = 3300.0 nM 5.48
CHEMBL294264 PURPURIN IC50 = 4000.0 nM 5.40
CHEMBL496 HEXACHLOROPHENE IC50 = 4700.0 nM 5.33
CHEMBL456 ETHACRYNIC ACID IC50 = 4700.0 nM 5.33
CHEMBL1265 ADAPALENE IC50 = 5100.0 nM 5.29
CHEMBL28626 MORIN IC50 = 5200.0 nM 5.28
CHEMBL506 PRIMAQUINE IC50 = 6200.0 nM 5.21
CHEMBL220190 ASCORBYL PALMITATE IC50 = 8500.0 nM 5.07
CHEMBL2003538 CETYLPYRIDINIUM CHLORIDE IC50 = 8900.0 nM 5.05
CHEMBL78764 IC50 = 8900.0 nM 5.05
CHEMBL5314343 IC50 = 12000.0 nM 4.92
CHEMBL290106 BITHIONOL IC50 = 13000.0 nM 4.89
CHEMBL64894 GENTIAN VIOLET IC50 = 15000.0 nM 4.82
CHEMBL265502 SURAMIN IC50 = 16000.0 nM 4.80
CHEMBL129177 HARMALOL IC50 = 16000.0 nM 4.80
CHEMBL1236460 THIOSTREPTON IC50 = 16000.0 nM 4.80
CHEMBL15594 ARACHIDONIC ACID IC50 = 18000.0 nM 4.75
CHEMBL1534 RIBOFLAVIN IC50 = 18000.0 nM 4.75
CHEMBL38 TRETINOIN IC50 = 21000.0 nM 4.68
CHEMBL6067487 IVERMECTIN IC50 = 23000.0 nM 4.64
CHEMBL221753 BENZETHONIUM CHLORIDE IC50 = 26000.0 nM 4.58
CHEMBL153062 4-NONYLPHENOL IC50 = 29000.0 nM 4.54
CHEMBL34398 4'-METHOXYCHALCONE IC50 = 30000.0 nM 4.52
CHEMBL1042 CHOLECALCIFEROL IC50 = 31000.0 nM 4.51
CHEMBL1630577 ABAMECTIN COMPONENT B1A IC50 = 32000.0 nM 4.50
CHEMBL1879202 IC50 = 38000.0 nM 4.42
CHEMBL7747 4-HYDROXYCHALCONE IC50 = 40000.0 nM 4.40
CHEMBL1536 ERGOCALCIFEROL IC50 = 41000.0 nM 4.39
CHEMBL388590 BENZBROMARONE IC50 = 49000.0 nM 4.31
CHEMBL276473 4'-HYDROXYCHALCONE IC50 = 56000.0 nM 4.25
CHEMBL1478 LITHOCHOLIC ACID IC50 = 59000.0 nM 4.23
CHEMBL33845 DICHLOROPHEN IC50 = 66000.0 nM 4.18