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Compound Detail

CHEMBL4213304

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COc1ccc2ncc(C(=O)N3CCN(S(C)(=O)=O)CC3)c(N3CCC(C#N)(c4ccccc4)CC3)c2c1

Basic Information

ChEMBL ID CHEMBL4213304
Phase Preclinical
Structure Type MOL
InChI Key LXZPTKHHMFQKBR-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

533.6
MW (Da)
3.02
ALogP
7
HBA
0
HBD
106.8
PSA (Ų)
0.50
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31N5O4S
MW 533.65
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.32

Activity Summary

IC50 2 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aldehyde dehydrogenase 1A1
CHEMBL3577
IC50 7.92 7.71 12.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.06667 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29767973 10.1021/acs.jmedchem.8b00270 Aldehyde dehydrogenase 1A1 2
29767973 10.1021/acs.jmedchem.8b00270 ADMET 1

Data from ChEMBL 36 via Core Engine