Compound Detail
CHEMBL2103758
PRAMLINTIDE 💊 Approved Drug
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💊 Approved Drug
CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)[C@@H](C)O
Basic Information
| ChEMBL ID | CHEMBL2103758 |
| Name | PRAMLINTIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | TZIRZGBAFTZREM-MKAGXXMWSA-N |
| Therapeutic | ✓ Yes |
9
Targets
22
Activities
2
Assay Types
2
PK Parameters
11
Publications
7
Known Names
4
Indications
Molecular Properties
3949.4
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2005 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Diabetes Mellitus Diabetes Mellitus, Type 1 Diabetes Mellitus, Type 2 Obesity
ATC Classification
A10BX05
pramlintide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
EC50 14 meas. best 10.66
IC50 8 meas. best 9.94
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Amylin receptor AMY1, CALCR/RAMP1 CHEMBL2111189 | EC50 | 10.66 | 10.66 | 0.0 | 1 |
| Amylin receptor AMY3; CALCR/RAMP3 CHEMBL2111190 | EC50 | 10.53 | 10.53 | 0.0 | 1 |
| Amylin receptor AMY2; CALCR/RAMP2 CHEMBL2364173 | EC50 | 10.19 | 10.19 | 0.1 | 1 |
| Calcitonin receptor CHEMBL1832 | EC50 | 10.15 | 9.815 | 0.1 | 2 |
| Unchecked CHEMBL612545 | EC50 | 10.15 | 9.445 | 0.1 | 2 |
| Amylin receptor AMY3; CALCR/RAMP3 CHEMBL2111190 | IC50 | 9.94 | 9.94 | 0.1 | 1 |
| Unchecked CHEMBL612545 | IC50 | 9.94 | 9.2275 | 0.1 | 4 |
| Amylin receptor AMY3; CALCR/RAMP3 CHEMBL2109235 | IC50 | 9.91 | 9.91 | 0.1 | 1 |
| Calcitonin receptor CHEMBL1832 | IC50 | 8.83 | 8.83 | 1.5 | 1 |
| Calcitonin receptor CHEMBL2204 | EC50 | 8.74 | 8.74 | 1.8 | 1 |
| Calcitonin receptor CHEMBL2204 | IC50 | 8.23 | 8.23 | 5.8 | 1 |
| Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 CHEMBL2107838 | EC50 | 7.63 | 7.63 | 23.4 | 1 |
| Adrenomedullin receptor, AM2; CALCRL/RAMP3 CHEMBL2111191 | EC50 | 6.83 | 6.83 | 147.9 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| F | 30.0 | % | Homo sapiens |
| T1/2 | 0.8 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 34288673 | 10.1021/acs.jmedchem.1c00565 | Unchecked | 12 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Amylin receptor AMY3; CALCR/RAMP3 | 5 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Calcitonin receptor | 5 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Unchecked | 4 |
| 26948801 | 10.1016/j.drudis.2016.02.015 | Homo sapiens | 2 |
| 38691890 | 10.1016/j.ejmech.2024.116456 | ADMET | 2 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Amylin receptor AMY1, CALCR/RAMP1 | 1 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Amylin receptor AMY2; CALCR/RAMP2 | 1 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 | 1 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Adrenomedullin receptor AM1; CALCRL/RAMP2 | 1 |
| 38960379 | 10.1021/acs.jmedchem.4c00022 | Adrenomedullin receptor, AM2; CALCRL/RAMP3 | 1 |
Data from ChEMBL 36 via Core Engine