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Compound Detail

CHEMBL3775578

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CC(=O)NCCNc1ccc2[nH]nc(Cc3ccc(-c4cnn(C)c4)cc3)c2c1

Basic Information

ChEMBL ID CHEMBL3775578
Phase Preclinical
Structure Type MOL
InChI Key CISPMBXZQNYLKC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

388.5
MW (Da)
3.10
ALogP
5
HBA
3
HBD
87.6
PSA (Ų)
0.42
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N6O
MW 388.48
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.66

Activity Summary

IC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK8/Cyclin C
CHEMBL3038474
IC50 6.17 6.17 680.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.0 mL.min-1.g-1 Homo sapiens
CL 14.0 mL.min-1.g-1 Rattus norvegicus
CL 37.0 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK8/Cyclin C IC50 = 680.0 nM 6.17 Displacement of dye-labeled ATP competitive probe from recombinant human CDK8/Cy... 26852363

Literature References

PubMed DOI Target Context # Activities
26852363 10.1016/j.bmcl.2016.01.062 Liver microsome 2
26852363 10.1016/j.bmcl.2016.01.062 CDK8/Cyclin C 1
26852363 10.1016/j.bmcl.2016.01.062 Cyclin-dependent kinase 8 1
26852363 10.1016/j.bmcl.2016.01.062 ADMET 1
26852363 10.1016/j.bmcl.2016.01.062 No relevant target 1

Data from ChEMBL 36 via Core Engine