Compound Detail
CHEMBL2001019
PF-04217903 Phase I
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Phase I
Basic Information
| ChEMBL ID | CHEMBL2001019 |
| Name | PF-04217903 |
| Phase | Phase I |
| Structure Type | MOL |
| InChI Key | PDMUGYOXRHVNMO-UHFFFAOYSA-N |
14
Targets
68
Activities
4
Assay Types
7
PK Parameters
20
Publications
3
Known Names
1
Indications
1
Mechanisms
Molecular Properties
372.4
MW (Da)
1.67
ALogP
9
HBA
1
HBD
107.4
PSA (Ų)
0.50
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Hepatocyte growth factor receptor inhibitor | INHIBITOR | Hepatocyte growth factor receptor | ✓ | ✓ |
Indications
Neoplasms
Activity Summary
IC50 49 meas. best 8.51
Ki 15 meas. best 9.2
Kd 3 meas. best 8.7
EC50 1 meas. best 9.52
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Hepatocyte growth factor receptor CHEMBL3717 | EC50 | 9.52 | 9.52 | 0.3 | 1 |
| Hepatocyte growth factor receptor CHEMBL3717 | Ki | 9.2 | 7.2085 | 0.6 | 13 |
| Hepatocyte growth factor receptor CHEMBL3717 | Kd | 8.7 | 8.4667 | 2.0 | 3 |
| Hepatocyte growth factor receptor CHEMBL3717 | IC50 | 8.51 | 8.0476 | 3.1 | 25 |
| Unchecked CHEMBL612545 | IC50 | 8.19 | 8.0533 | 6.4 | 6 |
| Hepatocyte growth factor receptor CHEMBL5585 | IC50 | 8.16 | 8.16 | 6.9 | 1 |
| HT-29 CHEMBL384 | IC50 | 8.15 | 8.15 | 7.0 | 1 |
| HUVEC CHEMBL613979 | IC50 | 8.14 | 7.8733 | 7.3 | 3 |
| Hepatocyte growth factor receptor CHEMBL2046265 | IC50 | 8.02 | 8.02 | 9.5 | 1 |
| NCI-H441 CHEMBL1075542 | IC50 | 7.96 | 7.93 | 11.0 | 2 |
| GTL 16 cell line CHEMBL612708 | IC50 | 7.92 | 7.715 | 12.0 | 2 |
| Unchecked CHEMBL612545 | Ki | 7.89 | 7.65 | 13.0 | 2 |
| NCI-H1993 CHEMBL1075527 | IC50 | 7.52 | 7.495 | 30.0 | 2 |
| Phosphodiesterase 3 CHEMBL2094125 | IC50 | 5.89 | 5.525 | 1300.0 | 2 |
| cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A CHEMBL4409 | IC50 | 5.57 | 5.57 | 2700.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 5.3 | 5.3 | 5000.0 | 1 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B CHEMBL290 | IC50 | 5.27 | 5.27 | 5360.0 | 1 |
| cGMP-specific 3',5'-cyclic phosphodiesterase CHEMBL2304402 | IC50 | 5.09 | 5.09 | 8060.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 8.2 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 1.48 | mL.min-1.g-1 | Homo sapiens |
| F | 71.0 | % | Rattus norvegicus |
| Fu | 0.16 | - | Homo sapiens |
| T1/2 | 3.7 | hr | Rattus norvegicus |
| T1/2 | 2.7 | hr | Homo sapiens |
| T1/2 | 0.05 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine