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Compound Detail

CHEMBL4126939

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Cc1cccc(OC[C@H](O)CN2CCN(CCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1C

Basic Information

ChEMBL ID CHEMBL4126939
Phase Preclinical
Structure Type MOL
InChI Key ZMHIBBAZRKTBAY-HSZRJFAPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
3.11
ALogP
6
HBA
1
HBD
73.3
PSA (Ų)
0.49
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33N3O4
MW 487.60
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.98

Activity Summary

EC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L-lactate dehydrogenase A chain
CHEMBL4835
EC50 6.17 6.17 670.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
L-lactate dehydrogenase A chain EC50 = 670.0 nM 6.17 Inhibition of human LDH5 using pyruvate as substrate after 10 mins 29861142

Literature References

PubMed DOI Target Context # Activities
29861142 10.1016/j.bmcl.2018.05.052 L-lactate dehydrogenase A chain 2
29861142 10.1016/j.bmcl.2018.05.052 MG-63 2

Data from ChEMBL 36 via Core Engine