Compound Detail
CHEMBL3785909
AMG-337 🧪 Phase II
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🧪 Phase II
COCCOc1cnc2ccn([C@H](C)c3nnc4c(F)cc(-c5cnn(C)c5)cn34)c(=O)c2c1
Basic Information
| ChEMBL ID | CHEMBL3785909 |
| Name | AMG-337 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | DWHXUGDWKAIASB-CQSZACIVSA-N |
1
Targets
2
Activities
1
Assay Types
17
PK Parameters
13
Publications
2
Known Names
7
Indications
1
Mechanisms
Molecular Properties
463.5
MW (Da)
2.61
ALogP
10
HBA
0
HBD
101.4
PSA (Ų)
0.34
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Hepatocyte growth factor receptor inhibitor | INHIBITOR | Hepatocyte growth factor receptor | ✓ | ✓ |
Indications
Neoplasms Neoplasms Sarcoma, Clear Cell Stomach Neoplasms Stomach Neoplasms Adenocarcinoma Esophageal Neoplasms
Activity Summary
IC50 2 meas. best 9.0
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Hepatocyte growth factor receptor CHEMBL3717 | IC50 | 9.0 | 8.65 | 1.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 21000.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 82600.0 | ng.hr.mL-1 | Canis lupus familiaris |
| CL | 26.67 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 4.5 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 6.0 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 8.0 | mL.min-1.g-1 | Mus musculus |
| CL | 9.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 3.833 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 7.667 | mL.min-1.kg-1 | Canis lupus familiaris |
| F | 30.0 | % | Rattus norvegicus |
| F | 49.0 | % | Canis lupus familiaris |
| F | 64.0 | % | Canis lupus familiaris |
| Fu | 0.174 | - | Rattus norvegicus |
| Fu | 0.366 | - | Mus musculus |
| Fu | 0.419 | - | Homo sapiens |
| T1/2 | 3.0 | hr | Rattus norvegicus |
| T1/2 | 5.9 | hr | Canis lupus familiaris |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Hepatocyte growth factor receptor | IC50 | = | 1.0 | nM | 9.0 | Inhibition of recombinant MET (unknown origin) using gastrin peptide as substrat... | 26812066 |
| Hepatocyte growth factor receptor | IC50 | = | 5.0 | nM | 8.3 | Inhibition of HGF-mediated MET autophosphorylation in human PC3 cells preincubat... | 26812066 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Canis familiaris | 8 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Mus musculus | 7 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Rattus norvegicus | 5 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | NON-PROTEIN TARGET | 3 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Hepatocyte growth factor receptor | 2 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Molecular identity unknown | 2 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Liver microsome | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | Plasma | 1 |
| 26812066 | 10.1021/acs.jmedchem.5b01716 | ADMET | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine