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Compound Detail

CHEMBL3747108

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

Basic Information

ChEMBL ID CHEMBL3747108
Phase Preclinical
Structure Type MOL
InChI Key FXUVMEINVSOBBC-UHFFFAOYSA-N
5
Targets
12
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

451.5
MW (Da)
4.87
ALogP
5
HBA
1
HBD
94.8
PSA (Ų)
0.47
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N5O2
MW 451.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.14

Activity Summary

IC50 12 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SRSF protein kinase 1
CHEMBL4375
IC50 8.32 8.32 4.8 1
SRSF protein kinase 2
CHEMBL5668
IC50 7.63 7.63 23.6 1
EML4-ALK
CHEMBL3883330
IC50 7.6 6.945 25.0 8
Unchecked
CHEMBL612545
IC50 6.2 6.2 628.0 1
ADMET
CHEMBL612558
IC50 5.78 5.78 1647.0 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
26568289 10.1021/acs.jmedchem.5b01136 Unchecked 1

Data from ChEMBL 36 via Core Engine