Compound Detail
CHEMBL489095
CAMICINAL 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL489095 |
| Name | CAMICINAL |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | RZKDEGZIFSJVNA-IBGZPJMESA-N |
5
Targets
8
Activities
2
Assay Types
8
PK Parameters
20
Publications
5
Known Names
1
Indications
1
Mechanisms
Molecular Properties
424.6
MW (Da)
3.27
ALogP
4
HBA
2
HBD
47.6
PSA (Ų)
0.75
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Motilin receptor agonist | AGONIST | Motilin receptor | ✓ | ✓ |
Indications
Gastroparesis
Activity Summary
EC50 4 meas. best 7.9
IC50 4 meas. best 4.8
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Motilin receptor CHEMBL2203 | EC50 | 7.9 | 6.955 | 12.6 | 2 |
| Unchecked CHEMBL612545 | EC50 | 7.38 | 7.23 | 42.0 | 2 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 4.8 | 4.8 | 15848.9 | 1 |
| Cytochrome P450 3A4 CHEMBL340 | IC50 | 4.58 | 4.37 | 26000.0 | 2 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 4.47 | 4.47 | 34000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 200040000.0 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 0.6 | mL.min-1.g-1 | Homo sapiens |
| CL | 1.0 | mL.min-1.g-1 | Rattus norvegicus |
| Cmax | 400.0 | nM | Rattus norvegicus |
| F | 48.0 | % | Rattus norvegicus |
| F | 51.0 | % | Canis lupus familiaris |
| T1/2 | 0.7817 | hr | Oryctolagus cuniculus |
| Tmax | 2.0 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Motilin receptor | EC50 | = | 12.59 | nM | 7.9 | Agonist activity at human recombinant motilin receptor expressed in CHO cells as... | 19191554 |
| Unchecked | EC50 | = | 42.0 | nM | 7.38 | Agonist activity at rabbit GPR38 expressed in COS-7 cells | 35051575 |
| Unchecked | EC50 | = | 82.6 | nM | 7.08 | Ex vivo agonist activity at GPR38 in rabbit duodenum muscle tissue assessed as i... | 35051575 |
| Motilin receptor | EC50 | = | 970.0 | nM | 6.01 | Agonist activity at human GPR38 expressed in COS-7 cells | 35051575 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 15848.93 | nM | 4.8 | Binding affinity to human ERG | 19191554 |
| Cytochrome P450 3A4 | IC50 | = | 26000.0 | nM | 4.58 | Inhibition of human CYP3A4 expressed in Escherichia coli using diethoxyfluoresce... | 19191554 |
| Cytochrome P450 2D6 | IC50 | = | 34000.0 | nM | 4.47 | Inhibition of human CYP2D6 | 19191554 |
| Cytochrome P450 3A4 | IC50 | = | 69000.0 | nM | 4.16 | Inhibition of human CYP3A4 expressed in Escherichia coli using 7BQ substrate by ... | 19191554 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 19191554 | 10.1021/jm801332q | Rattus norvegicus | 5 |
| 19191554 | 10.1021/jm801332q | Stomach | 4 |
| 19191554 | 10.1021/jm801332q | Cytochrome P450 3A4 | 3 |
| 19191554 | 10.1021/jm801332q | Motilin receptor | 2 |
| 35051575 | 10.1016/j.bmcl.2022.128554 | Unchecked | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 19191554 | 10.1021/jm801332q | Plasma | 2 |
| 19191554 | 10.1021/jm801332q | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 19191554 | 10.1021/jm801332q | ADMET | 1 |
| 19191554 | 10.1021/jm801332q | Growth hormone secretagogue receptor type 1 | 1 |
| 19191554 | 10.1021/jm801332q | Homo sapiens | 1 |
| 19191554 | 10.1021/jm801332q | Cytochrome P450 2D6 | 1 |
| 19191554 | 10.1021/jm801332q | Cytochrome P450 2C19 | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| 19191554 | 10.1021/jm801332q | Cytochrome P450 2C9 | 1 |
| 19191554 | 10.1021/jm801332q | Cytochrome P450 1A2 | 1 |
| 35051575 | 10.1016/j.bmcl.2022.128554 | Motilin receptor | 1 |
| 19191554 | 10.1021/jm801332q | Canis familiaris | 1 |
Data from ChEMBL 36 via Core Engine