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Compound Detail

CHEMBL72147

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Cc1cnc2c(Br)c(NC3=NCCN3)ccc2n1

Basic Information

ChEMBL ID CHEMBL72147
Phase Preclinical
Structure Type MOL
InChI Key ICROYPJYNVAMQF-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

306.2
MW (Da)
2.07
ALogP
5
HBA
2
HBD
62.2
PSA (Ų)
0.85
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H12BrN5
MW 306.17
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.74

Activity Summary

Ki 4 meas. best 7.13
EC50 2 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 7.13 7.13 74.1 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.49 6.49 323.6 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.19 6.19 645.6 1
Alpha-2C adrenergic receptor
CHEMBL1916
EC50 6.08 6.08 831.8 1
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 6.07 6.07 851.1 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 5.3 5.3 5011.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00391-6 Alpha-2A adrenergic receptor 3
- 10.1016/0960-894X(95)00391-6 Alpha-2B adrenergic receptor 3
- 10.1016/0960-894X(95)00391-6 Alpha-2C adrenergic receptor 3
- 10.1016/0960-894X(95)00391-6 Alpha-1A adrenergic receptor 1
- 10.1016/0960-894X(95)00391-6 Alpha-1B adrenergic receptor 1
- 10.1016/0960-894X(95)00391-6 Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine