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Compound Detail

CHEMBL3597011

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CN1CCc2cc(-c3cnc4[nH]cc(C(=O)c5ccccc5Cl)c4c3)ccc2C1

Basic Information

ChEMBL ID CHEMBL3597011
Phase Preclinical
Structure Type MOL
InChI Key UOQSDEILBQECQK-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
1
PK Parameters
20
Publications
0
Known Names

Molecular Properties

401.9
MW (Da)
5.10
ALogP
3
HBA
1
HBD
49.0
PSA (Ų)
0.49
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 C24H20ClN3O
MW 401.90
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.78

Activity Summary

IC50 3 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase N1
CHEMBL3384
IC50 9.0 9.0 1.0 1
Serine/threonine-protein kinase PAK 1
CHEMBL4600
IC50 9.0 7.925 1.0 2

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.035 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00280F Unchecked 3
25415869 10.1021/jm501613q Unchecked 3
25415869 10.1021/jm501613q Serine/threonine-protein kinase N1 3
- 10.1039/C4MD00280F Serine/threonine-protein kinase PAK 1 3
25415869 10.1021/jm501613q Tyrosine-protein kinase Lyn 2
- 10.1039/C4MD00280F No relevant target 1
25415869 10.1021/jm501613q Serine/threonine-protein kinase B-raf 1
25415869 10.1021/jm501613q Aurora kinase A 1
25415869 10.1021/jm501613q Serine/threonine-protein kinase WNK2 1
25415869 10.1021/jm501613q Tyrosine-protein kinase ABL1 1
25415869 10.1021/jm501613q RAC-alpha serine/threonine-protein kinase 1
25415869 10.1021/jm501613q Activin receptor type-1B 1
- 10.1039/C4MD00280F Plasma 1
- 10.1039/C4MD00280F Tyrosine-protein kinase Yes 1
- 10.1039/C4MD00280F Proto-oncogene tyrosine-protein kinase Src 1
- 10.1039/C4MD00280F Proto-oncogene tyrosine-protein kinase receptor Ret 1
- 10.1039/C4MD00280F Protein-tyrosine kinase 6 1
- 10.1039/C4MD00280F Tyrosine-protein kinase Lyn 1
- 10.1039/C4MD00280F Tyrosine-protein kinase Lck 1
- 10.1039/C4MD00280F Tyrosine-protein kinase Fyn 1

Data from ChEMBL 36 via Core Engine