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Compound Detail

CHEMBL143587

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

Basic Information

ChEMBL ID CHEMBL143587
Phase Preclinical
Structure Type MOL
InChI Key YOBMIXIISZAQGF-QTJFZDIUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

516.4
MW (Da)
5.23
ALogP
6
HBA
2
HBD
83.5
PSA (Ų)
0.44
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 C23H22F6N4O3
MW 516.44
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 10.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
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 Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed... 9804700

Literature References

PubMed DOI Target Context # Activities
9804700 10.1021/jm980299k Gerbillinae 3
9804700 10.1021/jm980299k Cavia porcellus 2
9804700 10.1021/jm980299k Substance-P receptor 1

Data from ChEMBL 36 via Core Engine