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Compound Detail

CHEMBL1780092

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Cc1oc(-c2ccccc2)nc1CN1CCC[C@@H](C(=O)NC[C@H]2CCCO2)C1

Basic Information

ChEMBL ID CHEMBL1780092
Phase Preclinical
Structure Type MOL
InChI Key NMRMEFHQDDESCE-RTBURBONSA-N

Known Names

PF-0458812900
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
1
Known Names

Molecular Properties

383.5
MW (Da)
3.16
ALogP
5
HBA
1
HBD
67.6
PSA (Ų)
0.83
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H29N3O3
MW 383.49
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.86

Activity Summary

IC50 1 meas. best 6.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
CHEMBL4408
IC50 6.78 6.78 166.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 84.0 mL.min-1.g-1 Homo sapiens
T1/2 0.1933 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B IC50 = 166.0 nM 6.78 Inhibition of PDE8B 21459572

Literature References

PubMed DOI Target Context # Activities
21459572 10.1016/j.bmcl.2011.03.022 Liver microsomes 2
21459572 10.1016/j.bmcl.2011.03.022 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B 1

Data from ChEMBL 36 via Core Engine