Compound Detail
CHEMBL2441929
ACOLTREMON 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL2441929 |
| Name | ACOLTREMON |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | HNSGVPAAXJJOPQ-XOKHGSTOSA-N |
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
15
Publications
5
Known Names
1
Indications
Molecular Properties
289.4
MW (Da)
4.34
ALogP
2
HBA
1
HBD
38.3
PSA (Ų)
0.89
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Indications
Dry Eye Syndromes
Activity Summary
EC50 2 meas. best 7.4
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Transient receptor potential cation channel subfamily M member 8 CHEMBL1075319 | EC50 | 7.4 | 6.16 | 40.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Transient receptor potential cation channel subfamily M member 8 | EC50 | = | 40.0 | nM | 7.4 | Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as... | 24080460 |
| Transient receptor potential cation channel subfamily M member 8 | EC50 | = | 12000.0 | nM | 4.92 | Agonist activity at TRPM8 (unknown origin) by fluorometric imaging plate reader ... | 27437828 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL5303304 | Fibroblast | 6 |
| - | 10.6019/CHEMBL5303304 | U2OS | 4 |
| 24080460 | 10.1016/j.bmcl.2013.09.016 | Transient receptor potential cation channel subfamily M member 8 | 1 |
| 27437828 | 10.1021/acs.jmedchem.6b00305 | Transient receptor potential cation channel subfamily M member 8 | 1 |
| - | 10.6019/CHEMBL5303304 | HEK-293T | 1 |
| - | 10.6019/CHEMBL5665443 | Methyl-CpG-binding domain protein 4 | 1 |
| - | 10.6019/CHEMBL5665443 | DNA-3-methyladenine glycosylase | 1 |
| - | 10.6019/CHEMBL5665443 | Adenine DNA glycosylase | 1 |
| - | 10.6019/CHEMBL5665443 | Endonuclease 8-like 1 | 1 |
| - | 10.6019/CHEMBL5665443 | Endonuclease 8-like 2 | 1 |
| - | 10.6019/CHEMBL5665443 | Endonuclease III-like protein 1 | 1 |
| - | 10.6019/CHEMBL5665443 | N-glycosylase/DNA lyase | 1 |
| - | 10.6019/CHEMBL5665443 | Single-strand selective monofunctional uracil DNA glycosylase | 1 |
| - | 10.6019/CHEMBL5665443 | G/T mismatch-specific thymine DNA glycosylase | 1 |
| - | 10.6019/CHEMBL5665443 | Uracil-DNA glycosylase | 1 |
Data from ChEMBL 36 via Core Engine