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Compound Detail

CHEMBL4210711

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COc1ccccc1-c1ccc([C@H](C)Nc2cncc(N3C(=O)OC[C@@H]3C(C)C)n2)cc1

Basic Information

ChEMBL ID CHEMBL4210711
Phase Preclinical
Structure Type MOL
InChI Key ORFUGZARPBMXMB-LAUBAEHRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
5.31
ALogP
6
HBA
1
HBD
76.6
PSA (Ų)
0.55
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28N4O3
MW 432.52
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.72

Activity Summary

IC50 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kallikrein-6
CHEMBL4448
IC50 8.6 8.6 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Kallikrein-6 IC50 = 2.512 nM 8.6 Inhibition of KLK6 (unknown origin) 37252095

Literature References

PubMed DOI Target Context # Activities
29089260 10.1016/j.bmc.2017.10.009 Isocitrate dehydrogenase [NADP] cytoplasmic 4
29089260 10.1016/j.bmc.2017.10.009 HEK-293T 3
29089260 10.1016/j.bmc.2017.10.009 No relevant target 1
37252095 10.1039/d2md00415a Kallikrein-6 1

Data from ChEMBL 36 via Core Engine