Compound Detail
CHEMBL4297522
PEMIGATINIB 💊 Approved Drug
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💊 Approved Drug
CCN1C(=O)N(c2c(F)c(OC)cc(OC)c2F)Cc2cnc3[nH]c(CN4CCOCC4)cc3c21
Basic Information
| ChEMBL ID | CHEMBL4297522 |
| Name | PEMIGATINIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | HCDMJFOHIXMBOV-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
12
Targets
48
Activities
1
Assay Types
13
PK Parameters
20
Publications
5
Known Names
14
Indications
3
Mechanisms
Molecular Properties
487.5
MW (Da)
3.66
ALogP
6
HBA
1
HBD
83.2
PSA (Ų)
0.57
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2020 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Fibroblast growth factor receptor 2 inhibitor | INHIBITOR | Fibroblast growth factor receptor 2 | ✓ | ✓ |
| Fibroblast growth factor receptor 3 inhibitor | INHIBITOR | Fibroblast growth factor receptor 3 | ✓ | ✓ |
| Fibroblast growth factor receptor 1 inhibitor | INHIBITOR | Fibroblast growth factor receptor 1 | ✓ | ✓ |
Indications
Cholangiocarcinoma Neoplasms Neoplasms Breast Neoplasms Carcinoma, Non-Small-Cell Lung Colorectal Neoplasms Endometrial Neoplasms Liposarcoma Myeloproliferative Disorders Pancreatic Neoplasms Stomach Neoplasms Urinary Bladder Neoplasms Urogenital Neoplasms Leukemia, Myeloid, Acute
ATC Classification
L01EN02
pemigatinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 48 meas. best 10.0
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Fibroblast growth factor receptor 3 CHEMBL2742 | IC50 | 10.0 | 8.202 | 0.1 | 10 |
| Fibroblast growth factor receptor 1 CHEMBL3650 | IC50 | 9.4 | 8.7214 | 0.4 | 7 |
| Fibroblast growth factor receptor 2 CHEMBL4142 | IC50 | 9.4 | 8.7 | 0.4 | 7 |
| Unchecked CHEMBL612545 | IC50 | 8.59 | 7.6433 | 2.6 | 3 |
| KATO III stomach cancer cell line CHEMBL612700 | IC50 | 8.51 | 8.51 | 3.1 | 1 |
| RT-112 CHEMBL614145 | IC50 | 8.48 | 7.362 | 3.3 | 5 |
| CC-LP-1 CHEMBL6066762 | IC50 | 8.44 | 6.9625 | 3.6 | 4 |
| SNU-16 CHEMBL613529 | IC50 | 8.41 | 8.32 | 3.9 | 2 |
| A204 CHEMBL614514 | IC50 | 7.74 | 7.74 | 18.4 | 1 |
| Fibroblast growth factor receptor 2 CHEMBL3648 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| Fibroblast growth factor receptor 4 CHEMBL3973 | IC50 | 7.57 | 7.455 | 27.0 | 6 |
| MDA-MB-453 CHEMBL614334 | IC50 | 7.13 | 7.13 | 73.7 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 3739.2 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3017.69 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 10773.97 | ng.hr.mL-1 | Canis lupus familiaris |
| CL | 8.0 | % | Macaca fascicularis |
| CL | 31.0 | % | Rattus norvegicus |
| CL | 10.0 | % | Canis lupus familiaris |
| F | 100.0 | % | Rattus norvegicus |
| F | 29.0 | % | Macaca fascicularis |
| F | 98.0 | % | Canis lupus familiaris |
| Fu | 0.11 | - | Homo sapiens |
| T1/2 | 4.0 | hr | Rattus norvegicus |
| T1/2 | 10.0 | hr | Macaca fascicularis |
| T1/2 | 15.7 | hr | Canis lupus familiaris |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine