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Compound Detail

CHEMBL1760199

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N#Cc1ccccc1N1CCN(C(=O)c2cc(-c3ccc(Cl)cc3)n[nH]2)CC1

Basic Information

ChEMBL ID CHEMBL1760199
Phase Preclinical
Structure Type MOL
InChI Key GPPCZGLJYWWKQI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

391.9
MW (Da)
3.56
ALogP
4
HBA
1
HBD
76.0
PSA (Ų)
0.74
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18ClN5O
MW 391.86
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -2.08

Activity Summary

IC50 1 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuromedin-K receptor
CHEMBL4429
IC50 6.32 6.32 480.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.3667 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuromedin-K receptor IC50 = 480.0 nM 6.32 Antagonist activity at human recombinant NK3 receptor expressed in CHO cells ass... 21376585

Literature References

PubMed DOI Target Context # Activities
21376585 10.1016/j.bmcl.2011.02.033 Neuromedin-K receptor 2
21376585 10.1016/j.bmcl.2011.02.033 Liver microsomes 1
21376585 10.1016/j.bmcl.2011.02.033 Plasma 1

Data from ChEMBL 36 via Core Engine