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Compound Detail

CHEMBL2204537

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CC(C)Oc1nc(-c2ccc(Cl)nc2)nc2c1CN(C(=O)c1cn(C)cn1)CC2.Cl

Basic Information

ChEMBL ID CHEMBL2204537
Phase Preclinical
Structure Type MOL
InChI Key SKCRWZXHSCTFFP-UHFFFAOYSA-N
Parent Compound CHEMBL2220083
Active Moiety CHEMBL2220083
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

412.9
MW (Da)
2.91
ALogP
7
HBA
0
HBD
86.0
PSA (Ų)
0.61
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22Cl2N6O2
MW 449.34
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.74

Activity Summary

Ki 1 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
Ki 8.35 8.35 4.5 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.94 mL.min-1.kg-1 Canis lupus familiaris
CL 2.4 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A Ki = 4.5 nM 8.35 Inhibition of PDE10A 22892116

Literature References

PubMed DOI Target Context # Activities
22892116 10.1016/j.bmcl.2012.07.072 Rattus norvegicus 3
22892116 10.1016/j.bmcl.2012.07.072 Canis familiaris 1
22892116 10.1016/j.bmcl.2012.07.072 Plasma 1
22892116 10.1016/j.bmcl.2012.07.072 No relevant target 1
22892116 10.1016/j.bmcl.2012.07.072 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1

Data from ChEMBL 36 via Core Engine