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Compound Detail

CHEMBL374779

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C[C@@H](Nc1nccc(Cl)c1NC(=O)CC#N)c1ccc(-c2cccc(F)c2C#N)cc1

Basic Information

ChEMBL ID CHEMBL374779
Phase Preclinical
Structure Type MOL
InChI Key ZKNSQMRSBCQXFM-CQSZACIVSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

433.9
MW (Da)
5.44
ALogP
5
HBA
2
HBD
101.6
PSA (Ų)
0.54
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H17ClFN5O
MW 433.87
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.58

Activity Summary

Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B1 bradykinin receptor
CHEMBL4308
Ki 8.7 8.7 2.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.3 mL.min-1.kg-1 Rattus norvegicus
CL - - Canis lupus familiaris
F 80.0 % Rattus norvegicus
F - % Canis lupus familiaris
T1/2 0.9 hr Rattus norvegicus
t1/2 - - Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15588075 10.1021/jm049394l Rattus norvegicus 3
15588075 10.1021/jm049394l Canis familiaris 3
15588075 10.1021/jm049394l B1 bradykinin receptor 2

Data from ChEMBL 36 via Core Engine