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Compound Detail

CHEMBL1765684

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COc1ccc(-c2c(C)c(C(=O)NC3(C#N)CCCCC3)nn2-c2ccccc2Br)cc1

Basic Information

ChEMBL ID CHEMBL1765684
Phase Preclinical
Structure Type MOL
InChI Key VCKIDQVWSDVZCZ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

493.4
MW (Da)
5.58
ALogP
5
HBA
1
HBD
79.9
PSA (Ų)
0.50
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25BrN4O2
MW 493.41
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.12

Activity Summary

Ki 5 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cannabinoid receptor 1
CHEMBL218
Ki 7.8 7.8 15.7 1
Translocator protein
CHEMBL4552
Ki 6.55 6.55 279.0 1
Kappa-type opioid receptor
CHEMBL237
Ki 6.22 6.22 597.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.95 5.95 1130.0 1
Cannabinoid receptor 2
CHEMBL253
Ki 5.56 5.56 2750.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 1D 2
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 2A 2
21428406 10.1021/jm2000536 Unchecked 2
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 6 1
21428406 10.1021/jm2000536 D(1B) dopamine receptor 1
21428406 10.1021/jm2000536 D(1A) dopamine receptor 1
21428406 10.1021/jm2000536 Beta-3 adrenergic receptor 1
21428406 10.1021/jm2000536 Beta-1 adrenergic receptor 1
21428406 10.1021/jm2000536 Alpha-2C adrenergic receptor 1
21428406 10.1021/jm2000536 Alpha-2B adrenergic receptor 1
21428406 10.1021/jm2000536 Alpha-2A adrenergic receptor 1
21428406 10.1021/jm2000536 Alpha-1B adrenergic receptor 1
21428406 10.1021/jm2000536 Alpha-1A adrenergic receptor 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 7 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 5A 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 3A 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 2C 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 2B 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 1E 1
21428406 10.1021/jm2000536 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine