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Compound Detail

CHEMBL12609

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COc1ccc(NC(=O)c2cc(OCCCN(C)C)nn2Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL12609
Phase Preclinical
Structure Type MOL
InChI Key YZCSJBGQLATPMH-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
8
PK Parameters
7
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
3.52
ALogP
6
HBA
1
HBD
68.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28N4O3
MW 408.50
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.50

Activity Summary

IC50 2 meas. best 5.55
EC50 1 meas. best 5.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Homo sapiens
CHEMBL372
IC50 5.55 5.55 2840.0 2
Unchecked
CHEMBL612545
EC50 5.26 5.26 5490.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 61.1 ng.hr.mL-1 Rattus norvegicus
AUC 61.1 ng.hr.mL-1 Rattus norvegicus
Cmax 15.67 nM Rattus norvegicus
Cmax 15.67 nM Rattus norvegicus
F 12.0 % Rattus norvegicus
F 12.0 % Rattus norvegicus
Tmax 2.7 hr Rattus norvegicus
Tmax 2.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11327597 10.1016/s0960-894x(01)00141-x Rattus norvegicus 4
11141091 10.1021/jm001034k Rattus norvegicus 3
11327597 10.1016/s0960-894x(01)00141-x Homo sapiens 2
11141091 10.1021/jm001034k Unchecked 2
11327597 10.1016/s0960-894x(01)00141-x Unchecked 1
11141091 10.1021/jm001034k Homo sapiens 1
11141091 10.1021/jm001034k ADMET 1

Data from ChEMBL 36 via Core Engine