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Compound Detail

CHEMBL273693

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CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1

Basic Information

ChEMBL ID CHEMBL273693
Phase Preclinical
Structure Type MOL
InChI Key KUEXCKPCPBQTBU-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

507.4
MW (Da)
5.26
ALogP
5
HBA
2
HBD
85.2
PSA (Ų)
0.37
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23BrN4O3
MW 507.39
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.88

Activity Summary

IC50 4 meas. best 6.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gastrin/cholecystokinin type B receptor
CHEMBL2854
IC50 6.86 6.855 137.0 2
Cholecystokinin receptor type A
CHEMBL2871
IC50 6.01 6.01 980.0 2

Pharmacokinetic Data

Parameter Value Units Species
Ke 1300.0 nM -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00108-X Gastrin/cholecystokinin type B receptor 2
9544204 10.1021/jm970373j Gastrin/cholecystokinin type B receptor 1
9544204 10.1021/jm970373j Cholecystokinin receptor type A 1
9544204 10.1021/jm970373j Unchecked 1
- 10.1016/S0960-894X(97)00108-X Cholecystokinin receptor type A 1

Data from ChEMBL 36 via Core Engine