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Compound Detail

CHEMBL5408095

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[2H]C([2H])[C@]([2H])(c1cccc(-c2ncc(OCC3CCN(C)CC3)cn2)c1)n1nc(-c2cccc(C#N)c2)ccc1=O

Basic Information

ChEMBL ID CHEMBL5408095
Phase Preclinical
Structure Type MOL
InChI Key UIXLPSRJOFRUNA-DBJCDTFOSA-N
Parent Compound CHEMBL5499115
Active Moiety CHEMBL5499115
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
4.57
ALogP
8
HBA
0
HBD
96.9
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H30N6O2
MW 509.63
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.45

Activity Summary

IC50 1 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MHCC97H
CHEMBL4296470
IC50 7.43 7.43 37.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 103.73 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MHCC97H IC50 = 37.0 nM 7.43 Antiproliferative activity against human MHCC97H cells assessed as inhibition of... 37262349

Literature References

PubMed DOI Target Context # Activities
37262349 10.1021/acs.jmedchem.3c00028 MHCC97H 1
37262349 10.1021/acs.jmedchem.3c00028 ADMET 1

Data from ChEMBL 36 via Core Engine