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Compound Detail

CHEMBL62045

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Cc1ccc(C2(c3ccc(C)cc3)CC(=O)N(CCCN3CCC(C#N)(c4ccccc4Cl)CC3)C2=O)cc1

Basic Information

ChEMBL ID CHEMBL62045
Phase Preclinical
Structure Type MOL
InChI Key LDEQSIYHAXUIBH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

540.1
MW (Da)
5.95
ALogP
4
HBA
0
HBD
64.4
PSA (Ų)
0.35
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H34ClN3O2
MW 540.11
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.66

Activity Summary

Ki 3 meas. best 9.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.32 9.32 0.5 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.01 7.01 98.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.66 6.66 220.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 19.0 % Rattus norvegicus
F 11.0 % Canis lupus familiaris
T1/2 0.66 hr Rattus norvegicus
T1/2 1.7 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11459670 10.1016/s0960-894x(01)00320-1 Rattus norvegicus 2
11459670 10.1016/s0960-894x(01)00320-1 Canis familiaris 2
11459670 10.1016/s0960-894x(01)00320-1 Alpha-1A adrenergic receptor 1
11459670 10.1016/s0960-894x(01)00320-1 Alpha-1B adrenergic receptor 1
11459670 10.1016/s0960-894x(01)00320-1 Alpha-1D adrenergic receptor 1

Data from ChEMBL 36 via Core Engine