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Compound Detail

CHEMBL27926

NAPITANE
🧪 Phase II
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🧪 Phase II
c1ccc(C2CCN(CC3CCCc4c3ccc3c4OCO3)C2)cc1

Basic Information

ChEMBL ID CHEMBL27926
Name NAPITANE
Phase Phase II
Structure Type MOL
InChI Key HAEPGZUGYMHCJE-UHFFFAOYSA-N

Known Names

A-75200 Napitane Napitano
4
Targets
15
Activities
3
Assay Types
0
PK Parameters
3
Publications
3
Known Names

Molecular Properties

335.4
MW (Da)
4.32
ALogP
3
HBA
0
HBD
21.7
PSA (Ų)
0.83
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic
USAN Year 1996

Extended Properties

Molecular Formula C22H25NO2
MW 335.45
Aromatic Rings 2
Heavy Atoms 25

Activity Summary

Kd 6 meas. best 8.25
Ki 6 meas. best 9.37
IC50 3 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 9.37 9.1433 0.4 3
Adrenergic receptor alpha-2
CHEMBL2095158
Kd 8.25 8.19 5.6 3
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 7.84 7.7667 14.4 3
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.12 7.0133 75.9 3
Rattus norvegicus
CHEMBL376
IC50 6.08 5.8233 841.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adrenergic receptor alpha-2 Ki = 0.428 nM 9.37 In vitro binding affinity at Alpha-2 adrenergic receptor in rat cortex by radiol... -
Adrenergic receptor alpha-2 Ki = 0.708 nM 9.15 In vitro binding affinity at Alpha-2 adrenergic receptor in rat cortex by radiol... -
Adrenergic receptor alpha-2 Ki = 1.23 nM 8.91 In vitro binding affinity at Alpha-2 adrenergic receptor in rat cortex by radiol... -
Adrenergic receptor alpha-2 Kd = 5.623 nM 8.25 Evaluated for its postsynaptic Alpha-2 adrenergic receptor antagonist activity a... -
Adrenergic receptor alpha-2 Kd = 6.761 nM 8.17 Evaluated for its postsynaptic Alpha-2 adrenergic receptor antagonist activity a... -
Adrenergic receptor alpha-2 Kd = 7.079 nM 8.15 Evaluated for its postsynaptic Alpha-2 adrenergic receptor antagonist activity a... -
Adrenergic receptor alpha-2 Kd = 14.45 nM 7.84 Evaluated for its presynaptic Alpha-2 adrenergic receptor antagonistic activity ... -
Adrenergic receptor alpha-2 Kd = 16.6 nM 7.78 Evaluated for its presynaptic Alpha-2 adrenergic receptor antagonistic activity ... -
Adrenergic receptor alpha-2 Kd = 20.89 nM 7.68 Evaluated for its presynaptic Alpha-2 adrenergic receptor antagonistic activity ... -
Adrenergic receptor alpha-1 Ki = 75.9 nM 7.12 In vitro binding affinity at Alpha-1 adrenergic receptor by radioligand binding ... -
Adrenergic receptor alpha-1 Ki = 106.0 nM 6.97 In vitro binding affinity at Alpha-1 adrenergic receptor by radioligand binding ... -
Adrenergic receptor alpha-1 Ki = 112.0 nM 6.95 In vitro binding affinity at Alpha-1 adrenergic receptor by radioligand binding ... -
Rattus norvegicus IC50 = 841.0 nM 6.08 Concentration required for its norepinephrine reuptake inhibitory activity in sy... -
Rattus norvegicus IC50 = 1320.0 nM 5.88 Concentration required for its norepinephrine reuptake inhibitory activity in sy... -
Rattus norvegicus IC50 = 3110.0 nM 5.51 Concentration required for its norepinephrine reuptake inhibitory activity in sy... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(01)80353-X Adrenergic receptor alpha-2 9
- 10.1016/S0960-894X(01)80353-X Adrenergic receptor alpha-1 3
- 10.1016/S0960-894X(01)80353-X Rattus norvegicus 3

Data from ChEMBL 36 via Core Engine