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Compound Detail

CHEMBL4217987

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O=C(Nc1ccc(O)cc1C(=O)O)c1ccc(N2C(=O)c3ccccc3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL4217987
Phase Preclinical
Structure Type MOL
InChI Key QRCGZVVZRATLQP-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

402.4
MW (Da)
3.14
ALogP
5
HBA
3
HBD
124.0
PSA (Ų)
0.45
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H14N2O6
MW 402.36
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.85

Activity Summary

IC50 3 meas. best 4.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NAD-dependent protein deacylase sirtuin-6
CHEMBL2163182
IC50 4.7 4.7 20000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.001 - Homo sapiens
Fu 0.001 - Homo sapiens
Fu 0.01 - Mus musculus
Fu 0.01 - Mus musculus
T1/2 7.7 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28958848 10.1016/j.bmc.2017.09.023 No relevant target 6
28958848 10.1016/j.bmc.2017.09.023 NAD-dependent protein deacylase sirtuin-6 5
28958848 10.1016/j.bmc.2017.09.023 ADMET 5
28958848 10.1016/j.bmc.2017.09.023 Unchecked 2
28958848 10.1016/j.bmc.2017.09.023 NAD-dependent protein deacetylase sirtuin-1 1
28958848 10.1016/j.bmc.2017.09.023 NAD-dependent protein deacetylase sirtuin-2 1

Data from ChEMBL 36 via Core Engine