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Compound Detail

CHEMBL2425544

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C=C(C)[C@]12C[C@@H](C)[C@@]34O[C@](Cc5ccccc5)(O[C@@H]1[C@@H]3C=C(COC(=O)Oc1cc(F)c(N)c(OC)c1)C[C@]1(O)C(=O)C(C)=C[C@@H]41)O2

Basic Information

ChEMBL ID CHEMBL2425544
Phase Preclinical
Structure Type MOL
InChI Key JOQWVMCVMXGTEL-GGBXHWPASA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

647.7
MW (Da)
5.19
ALogP
10
HBA
2
HBD
135.8
PSA (Ų)
0.18
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H38FNO9
MW 647.70
Aromatic Rings 2
Heavy Atoms 47
NP-Likeness 2.16

Activity Summary

EC50 2 meas. best 8.5
Ki 2 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
Ki 8.66 8.66 2.2 1
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
EC50 8.5 8.5 3.2 1
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
EC50 7.75 7.75 17.9 1
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
Ki 6.08 6.08 830.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23981530 10.1016/j.ejmech.2013.07.042 Transient receptor potential cation channel subfamily V member 1 10

Data from ChEMBL 36 via Core Engine