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Compound Detail

CHEMBL189478

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CC(C)[C@@H](N)C(=O)OC[n+]1ccc(N/C(=N/CCCCCCOc2ccc(Cl)cc2)NC#N)cc1.Cl.[Cl-]

Basic Information

ChEMBL ID CHEMBL189478
Phase Preclinical
Structure Type MOL
InChI Key CAVWZDUEUBYNLK-MQWQBNKOSA-N
Parent Compound CHEMBL1626639
Active Moiety CHEMBL1626639
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

502.0
MW (Da)
3.59
ALogP
6
HBA
3
HBD
125.6
PSA (Ų)
0.07
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H35Cl3N6O3
MW 573.95
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.43

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NSCLC
CHEMBL612554
IC50 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 - hr -
T1/2 - hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NSCLC IC50 = 5.012 nM 8.3 Inhibition of NYH Cell line 15863303

Literature References

PubMed DOI Target Context # Activities
15863303 10.1016/j.bmcl.2005.03.064 No relevant target 2
15863303 10.1016/j.bmcl.2005.03.064 ADMET 2
15863303 10.1016/j.bmcl.2005.03.064 NSCLC 1

Data from ChEMBL 36 via Core Engine