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Compound Detail

CHEMBL1086684

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CCC(C)(C)Cc1c[nH]c(CCc2ccc(-c3ccccc3OCc3nc(=O)[nH][nH]3)cc2)n1

Basic Information

ChEMBL ID CHEMBL1086684
Phase Preclinical
Structure Type MOL
InChI Key GYPRMKOUJUFZMB-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

445.6
MW (Da)
4.83
ALogP
4
HBA
3
HBD
99.5
PSA (Ų)
0.33
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 C26H31N5O2
MW 445.57
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.41

Activity Summary

EC50 1 meas. best 6.47
IC50 1 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bombesin receptor subtype-3
CHEMBL4080
IC50 7.51 7.51 31.0 1
Bombesin receptor subtype-3
CHEMBL4080
EC50 6.47 6.47 336.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bombesin receptor subtype-3 IC50 = 31.0 nM 7.51 Binding affinity to human BRS3 20347296
Bombesin receptor subtype-3 EC50 = 336.0 nM 6.47 Agonist activity at human BRS3 20347296

Literature References

PubMed DOI Target Context # Activities
20347296 10.1016/j.bmcl.2010.03.028 Bombesin receptor subtype-3 5

Data from ChEMBL 36 via Core Engine