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Compound Detail

CHEMBL1822522

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COc1cc(N2CCN(N3CCOCC3)CC2)ccc1Nc1ncc2ccc(-c3ccccc3OC)n2n1

Basic Information

ChEMBL ID CHEMBL1822522
Phase Preclinical
Structure Type MOL
InChI Key ZCIQMENOTTVELZ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

515.6
MW (Da)
3.53
ALogP
10
HBA
1
HBD
79.6
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H33N7O3
MW 515.62
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.20

Activity Summary

IC50 3 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ALK tyrosine kinase receptor
CHEMBL4247
IC50 8.05 8.05 9.0 1
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor)
CHEMBL2111387
IC50 7.07 7.07 85.0 1
Insulin receptor
CHEMBL1981
IC50 6.45 6.45 357.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 34.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21859094 10.1021/jm200758k NON-PROTEIN TARGET 3
21859094 10.1021/jm200758k Mus musculus 3
21859094 10.1021/jm200758k ALK tyrosine kinase receptor 1
21859094 10.1021/jm200758k NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor) 1
21859094 10.1021/jm200758k Insulin receptor 1
21859094 10.1021/jm200758k Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine