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Compound Detail

CHEMBL72107

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Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCN1C

Basic Information

ChEMBL ID CHEMBL72107
Phase Preclinical
Structure Type MOL
InChI Key YWMWOFSCNNTOND-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
4
PK Parameters
9
Publications
0
Known Names

Molecular Properties

258.4
MW (Da)
3.49
ALogP
2
HBA
0
HBD
15.6
PSA (Ų)
0.79
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 C17H26N2
MW 258.41
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.48

Activity Summary

Ki 3 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 7.07 7.07 86.0 2
Adrenergic receptor alpha-2
CHEMBL2095158
Ki 5.88 5.88 1320.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 66.4 mL.min-1.kg-1 Rattus norvegicus
F 42.1 % Rattus norvegicus
T1/2 0.95 hr Rattus norvegicus
Vd 3.974 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15324890 10.1016/j.bmcl.2004.06.085 ADMET 4
9632357 10.1021/jm970513p 5-hydroxytryptamine receptor 1B 1
9632357 10.1021/jm970513p 5-hydroxytryptamine receptor 1D 1
9632357 10.1021/jm970513p Serotonin 1 receptors; 5-HT1B & 5-HT1D 1
9632357 10.1021/jm970513p Adrenergic receptor alpha 1
9632357 10.1021/jm970513p Adrenergic receptor alpha-2 1
15324890 10.1016/j.bmcl.2004.06.085 5-hydroxytryptamine receptor 1B 1
15324890 10.1016/j.bmcl.2004.06.085 5-hydroxytryptamine receptor 1D 1
15324890 10.1016/j.bmcl.2004.06.085 Oryctolagus cuniculus 1

Data from ChEMBL 36 via Core Engine