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Compound Detail

CHEMBL373535

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CC(Oc1ccccc1-c1cccnc1)C1=NCCN1

Basic Information

ChEMBL ID CHEMBL373535
Phase Preclinical
Structure Type MOL
InChI Key AFWQDDUMQAQVSC-UHFFFAOYSA-N
3
Targets
14
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

267.3
MW (Da)
2.52
ALogP
4
HBA
1
HBD
46.5
PSA (Ų)
0.93
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 C16H17N3O
MW 267.33
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.52

Activity Summary

EC50 8 meas. best 7.4
Ki 6 meas. best 7.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
EC50 7.4 7.3333 39.8 3
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.19 7.19 64.6 2
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.86 6.86 138.0 2
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 6.5 6.41 316.2 3
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.03 6.03 933.2 2
Alpha-2B adrenergic receptor
CHEMBL1942
EC50 6.0 6.0 1000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Alpha-2C adrenergic receptor EC50 = 39.81 nM 7.4 Agonist activity at human adrenergic Alpha-2C receptor expressed in CHO cells as... 15566287
Alpha-2C adrenergic receptor EC50 = 50.12 nM 7.3 Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells as... 15566287
Alpha-2C adrenergic receptor EC50 = 50.12 nM 7.3 Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells a... 17630725
Alpha-2C adrenergic receptor Ki = 64.57 nM 7.19 Displacement of [3H]RX821002 from human adrenergic Alpha-2C receptor expressed i... 15566287
Alpha-2C adrenergic receptor Ki = 64.57 nM 7.19 Displacement of [3H]RX 821002 from human adrenergic Alpha-2C receptor expressed ... 17630725
Alpha-2A adrenergic receptor Ki = 138.04 nM 6.86 Displacement of [3H]RX821002 from human adrenergic alpha2A receptor expressed in... 15566287
Alpha-2A adrenergic receptor Ki = 138.04 nM 6.86 Displacement of [3H]RX 821002 from human adrenergic alpha2A receptor expressed i... 17630725
Alpha-2A adrenergic receptor EC50 = 316.23 nM 6.5 Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells as... 15566287
Alpha-2A adrenergic receptor EC50 = 316.23 nM 6.5 Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells a... 17630725
Alpha-2A adrenergic receptor EC50 = 588.84 nM 6.23 Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells as... 15566287
Alpha-2B adrenergic receptor Ki = 933.25 nM 6.03 Displacement of [3H]RX821002 from human adrenergic alpha-2B receptor expressed i... 15566287
Alpha-2B adrenergic receptor Ki = 933.25 nM 6.03 Displacement of [3H]RX 821002 from human adrenergic alpha-2B receptor expressed ... 17630725
Alpha-2B adrenergic receptor EC50 = 1000.0 nM 6.0 Agonist activity at human adrenergic alpha-2B receptor expressed in CHO cells as... 15566287
Alpha-2B adrenergic receptor EC50 = 1000.0 nM 6.0 Agonistic potency at human adrenergic alpha-2B receptor expressed in CHO cells a... 17630725

Literature References

PubMed DOI Target Context # Activities
15566287 10.1021/jm0408215 Alpha-2A adrenergic receptor 5
15566287 10.1021/jm0408215 Alpha-2C adrenergic receptor 5
15566287 10.1021/jm0408215 Alpha-2B adrenergic receptor 3
17630725 10.1021/jm061487a Alpha-2A adrenergic receptor 3
17630725 10.1021/jm061487a Alpha-2B adrenergic receptor 3
17630725 10.1021/jm061487a Alpha-2C adrenergic receptor 3

Data from ChEMBL 36 via Core Engine