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Compound Detail

CHEMBL210365

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C[C@@H](O[C@H]1CCc2nnc(O)n2C[C@@H]1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL210365
Phase Preclinical
Structure Type MOL
InChI Key PRWFNQWPCVCDDH-DPMMWBKBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

503.4
MW (Da)
6.04
ALogP
5
HBA
1
HBD
60.2
PSA (Ų)
0.44
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20F7N3O2
MW 503.42
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.64

Activity Summary

IC50 1 meas. best 9.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.72 9.72 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.19 nM 9.72 Displacement of [125I] labeled substance P from human cloned NK1 receptor expres... 16574413

Literature References

PubMed DOI Target Context # Activities
16574413 10.1016/j.bmcl.2006.02.080 Substance-P receptor 1
16574413 10.1016/j.bmcl.2006.02.080 Voltage-gated inwardly rectifying potassium channel KCNH2 1
16574413 10.1016/j.bmcl.2006.02.080 Gerbil, jird 1

Data from ChEMBL 36 via Core Engine