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Compound Detail

CHEMBL275469

RWJ-38063
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CC(C)Oc1ccccc1N1CCN(CCNC(=O)CN2CCCCC2=O)CC1

Basic Information

ChEMBL ID CHEMBL275469
Name RWJ-38063
Phase Preclinical
Structure Type MOL
InChI Key IIRJWNCOXHFIBK-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

402.5
MW (Da)
1.72
ALogP
5
HBA
1
HBD
65.1
PSA (Ų)
0.72
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H34N4O3
MW 402.54
Aromatic Rings 1
Heavy Atoms 29
NP-Likeness -1.72

Activity Summary

Ki 4 meas. best 8.06
Kd 1 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.06 8.045 8.7 2
Rattus norvegicus
CHEMBL376
Kd 7.5 7.5 31.6 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.43 6.43 372.0 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 4.34 4.34 46120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10843225 10.1016/s0960-894x(00)00169-4 Alpha-1A adrenergic receptor 1
10843225 10.1016/s0960-894x(00)00169-4 Alpha-1B adrenergic receptor 1
10843225 10.1016/s0960-894x(00)00169-4 Alpha-1D adrenergic receptor 1
10843225 10.1016/s0960-894x(00)00169-4 Adrenergic receptors; alpha-1 A & B 1
10843225 10.1016/s0960-894x(00)00169-4 Alpha adrenergic receptor (1a and 1d) 1
10843225 10.1016/s0960-894x(00)00169-4 Rattus norvegicus 1
15664832 10.1016/j.bmcl.2004.11.032 Alpha-1A adrenergic receptor 1

Data from ChEMBL 36 via Core Engine