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Compound Detail

CHEMBL100636

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C[C@@H](O[C@H]1CCCN(Cc2n[nH]c(O)n2)[C@H]1c1ccccc1)c1cc(Cl)cc(Cl)c1

Basic Information

ChEMBL ID CHEMBL100636
Phase Preclinical
Structure Type MOL
InChI Key IBZJAXSAZUPUBI-RFVSGWPVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

447.4
MW (Da)
5.30
ALogP
5
HBA
2
HBD
74.3
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 C22H24Cl2N4O2
MW 447.37
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.76

Activity Summary

IC50 1 meas. best 10.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL4027
IC50 10.05 10.05 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.09 nM 10.05 Antagonism of NK1 receptor in rat liver microsomes. -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)10118-4 Unchecked 3
- 10.1016/S0960-894X(97)10118-4 Substance-P receptor 1

Data from ChEMBL 36 via Core Engine