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Compound Detail

CHEMBL358343

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C[C@@H](O[C@H]1OCCN(Cc2n[nH]c(O)n2)[C@H]1c1ccccc1)c1cccc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL358343
Phase Preclinical
Structure Type MOL
InChI Key BEQWHMKGQHGLOD-VOBQZIQPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

448.4
MW (Da)
4.21
ALogP
6
HBA
2
HBD
83.5
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23F3N4O3
MW 448.45
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.93

Activity Summary

IC50 1 meas. best 9.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.57 9.57 0.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.27 nM 9.57 Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed... 9804700

Literature References

PubMed DOI Target Context # Activities
9804700 10.1021/jm980299k Substance-P receptor 1

Data from ChEMBL 36 via Core Engine