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Compound Detail

CHEMBL4456001

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Cn1ncc2ccc(N3CCN(c4cncc5ccccc45)CC3)cc21

Basic Information

ChEMBL ID CHEMBL4456001
Phase Preclinical
Structure Type MOL
InChI Key RESKVYRMFBGCMT-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

343.4
MW (Da)
3.45
ALogP
5
HBA
0
HBD
37.2
PSA (Ų)
0.56
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N5
MW 343.43
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.30

Activity Summary

EC50 1 meas. best 6.92
Kd 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 8
CHEMBL5719
Kd 7.52 7.52 30.0 1
Unchecked
CHEMBL612545
EC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32071678 10.1021/acsmedchemlett.9b00480 ADMET 5
32071678 10.1021/acsmedchemlett.9b00480 Unchecked 2
32071678 10.1021/acsmedchemlett.9b00480 Cyclin-dependent kinase 8 1

Data from ChEMBL 36 via Core Engine