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Compound Detail

CHEMBL3734844

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CCc1cc2c(cc1-c1cnn(C3CCOCC3)c1)C(C)(C)c1[nH]c3cc(C#N)ccc3c1C2=O

Basic Information

ChEMBL ID CHEMBL3734844
Phase Preclinical
Structure Type MOL
InChI Key ZOUKGWPEJXISGG-UHFFFAOYSA-N
4
Targets
11
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

464.6
MW (Da)
5.69
ALogP
5
HBA
1
HBD
83.7
PSA (Ų)
0.42
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28N4O2
MW 464.57
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.09

Activity Summary

IC50 11 meas. best 7.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ALK tyrosine kinase receptor
CHEMBL4247
IC50 7.95 7.95 11.2 1
EML4-ALK
CHEMBL3883330
IC50 7.7 6.93 20.0 8
Unchecked
CHEMBL612545
IC50 6.21 6.21 620.0 1
ADMET
CHEMBL612558
IC50 6.03 6.03 924.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26568289 10.1021/acs.jmedchem.5b01136 EML4-ALK 10
26568289 10.1021/acs.jmedchem.5b01136 ADMET 2
26476749 10.1016/j.ejmech.2015.10.005 ALK tyrosine kinase receptor 1
26568289 10.1021/acs.jmedchem.5b01136 Unchecked 1

Data from ChEMBL 36 via Core Engine