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Compound Detail

CHEMBL184844

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CC(C)C1=NCCc2cc(C3CC3c3ccc4cc(C(=N)N)ccc4c3)ccc21

Basic Information

ChEMBL ID CHEMBL184844
Phase Preclinical
Structure Type MOL
InChI Key YNSGCLWGJIGXJS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
7
Publications
0
Known Names

Molecular Properties

381.5
MW (Da)
5.40
ALogP
2
HBA
2
HBD
62.2
PSA (Ų)
0.46
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N3
MW 381.52
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness 0.34

Activity Summary

Ki 1 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL3286
Ki 6.21 6.21 610.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 103.01 ng.hr.mL-1 Rattus norvegicus
F - % Rattus norvegicus
T1/2 0.33 hr Rattus norvegicus
Vd 7.9 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Urokinase-type plasminogen activator Ki = 610.0 nM 6.21 Binding affinity value against urokinase plasminogen activator 15582418

Literature References

PubMed DOI Target Context # Activities
15582418 10.1016/j.bmcl.2004.10.026 ADMET 5
15582418 10.1016/j.bmcl.2004.10.026 Urokinase-type plasminogen activator 1
15582418 10.1016/j.bmcl.2004.10.026 Tissue-type plasminogen activator 1
15582418 10.1016/j.bmcl.2004.10.026 Unchecked 1
15582418 10.1016/j.bmcl.2004.10.026 Plasminogen 1
15582418 10.1016/j.bmcl.2004.10.026 Kallikrein-1 1
15582418 10.1016/j.bmcl.2004.10.026 Trypsin 1

Data from ChEMBL 36 via Core Engine