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Compound Detail

CHEMBL5612634

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C=CC(=O)N(Cc1ccc(Cl)c(C#N)c1)c1ccc(O[C@@H]2CC[C@@H](N)C2)cc1

Basic Information

ChEMBL ID CHEMBL5612634
Phase Preclinical
Structure Type MOL
InChI Key DVAMTFVOOFYMOP-YLJYHZDGSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

395.9
MW (Da)
4.19
ALogP
4
HBA
1
HBD
79.3
PSA (Ų)
0.74
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22ClN3O2
MW 395.89
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.81

Activity Summary

EC50 1 meas. best 5.43
IC50 1 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcl-2-related protein A1
CHEMBL6044
IC50 6.46 6.46 350.0 1
Bcl-2-related protein A1
CHEMBL6044
EC50 5.43 5.43 3700.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.333 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39291659 10.1021/acs.jmedchem.4c01288 Bcl-2-related protein A1 2
39291659 10.1021/acs.jmedchem.4c01288 No relevant target 1
39291659 10.1021/acs.jmedchem.4c01288 ADMET 1

Data from ChEMBL 36 via Core Engine