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Assay Detail

CHEMBL4031659

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

Binding
Inhibition of human MDH1 expressed in Escherichia coli after 30 mins by oxaloacetate-dependent NADH oxidation assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Malate dehydrogenase, cytoplasmic (CHEMBL3560)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.
Naik R, Ban HS, Jang K, Kim I, Xu X, Harmalkar D, Shin SA, Kim M, Kim BK, Park J, Ku B, Oh S, Won M, Lee K.
J Med Chem (2017) 60 : 8631 -8646
PubMed 28991459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.50 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4096306 1 6.04
CHEMBL4068781 1 5.97
CHEMBL4065526 1 5.94
CHEMBL4091027 1 5.93
CHEMBL4098767 1 5.88
CHEMBL4074947 1 5.85
CHEMBL4074694 1 5.81
CHEMBL4068233 1 5.64
CHEMBL4087903 1 5.61
CHEMBL4099949 1 5.52
CHEMBL4095380 1 5.52
CHEMBL4073085 1 5.46
CHEMBL4086789 1 5.32
CHEMBL4080721 1 5.29
CHEMBL4105436 1 5.18
CHEMBL4085170 1 5.17
CHEMBL4078740 1 5.02
CHEMBL4095604 1 4.74
CHEMBL4069043 1 4.59
CHEMBL4079103 1 -
CHEMBL4103353 1 -
CHEMBL4059591 1 -
CHEMBL4087563 1 -
CHEMBL4067849 1 -
CHEMBL4060357 1 -
CHEMBL4089556 1 -
CHEMBL4086585 1 -
CHEMBL4076058 1 -
CHEMBL4073732 1 -
CHEMBL4090211 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4096306 IC50 = 920.0 nM 6.04
CHEMBL4068781 IC50 = 1070.0 nM 5.97
CHEMBL4065526 IC50 = 1140.0 nM 5.94
CHEMBL4091027 IC50 = 1180.0 nM 5.93
CHEMBL4098767 IC50 = 1310.0 nM 5.88
CHEMBL4074947 IC50 = 1400.0 nM 5.85
CHEMBL4074694 IC50 = 1540.0 nM 5.81
CHEMBL4068233 IC50 = 2270.0 nM 5.64
CHEMBL4087903 IC50 = 2430.0 nM 5.61
CHEMBL4099949 IC50 = 3000.0 nM 5.52
CHEMBL4095380 IC50 = 3000.0 nM 5.52
CHEMBL4073085 IC50 = 3440.0 nM 5.46
CHEMBL4086789 IC50 = 4740.0 nM 5.32
CHEMBL4080721 IC50 = 5160.0 nM 5.29
CHEMBL4105436 IC50 = 6650.0 nM 5.18
CHEMBL4085170 IC50 = 6790.0 nM 5.17
CHEMBL4078740 IC50 = 9580.0 nM 5.02
CHEMBL4095604 IC50 = 18350.0 nM 4.74
CHEMBL4069043 IC50 = 25960.0 nM 4.59
CHEMBL4079103 IC50 > 40000.0 nM -
CHEMBL4103353 IC50 > 40000.0 nM -
CHEMBL4059591 IC50 > 40000.0 nM -
CHEMBL4087563 IC50 > 40000.0 nM -
CHEMBL4067849 IC50 > 40000.0 nM -
CHEMBL4060357 IC50 > 40000.0 nM -
CHEMBL4089556 IC50 > 40000.0 nM -
CHEMBL4086585 IC50 > 40000.0 nM -
CHEMBL4076058 IC50 > 40000.0 nM -
CHEMBL4073732 IC50 > 40000.0 nM -
CHEMBL4090211 IC50 > 40000.0 nM -