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Compound Detail

CHEMBL1823872

SOMATOSTATIN
🧪 Phase III
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🧪 Phase III
C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1823872
Name SOMATOSTATIN
Phase Phase III
Structure Type BOTH
InChI Key NHXLMOGPVYXJNR-ATOGVRKGSA-N

Known Names

Somatostatin Somatostatin-14 Somatostatina Somatostatine SRIF-14
15
Targets
86
Activities
3
Assay Types
3
PK Parameters
20
Publications
5
Known Names
13
Indications
1
Mechanisms

Molecular Properties

1637.9
MW (Da)

Drug Information

Molecule Type Protein
Chirality Single Enantiomer

Flags

Natural Product
USAN Stem som-; -stat-

Extended Properties

Molecular Formula C76H104N18O19S2
MW 1637.91

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Somatostatin receptor agonist AGONIST Somatostatin receptor ✓ ✓

Indications

Carcinoma, Hepatocellular Gallbladder Neoplasms Hypertension, Portal Liver Failure Neuroendocrine Tumors Pancreatitis Polycystic Kidney, Autosomal Dominant Carcinoid Tumor Diabetes Mellitus, Type 1 Digestive System Diseases Peptic Ulcer Hypoglycemia Prostatic Neoplasms

ATC Classification

H01CB01
somatostatin
Level 1: SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
Level 2: PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES

Activity Summary

IC50 41 meas. best 10.13
Ki 41 meas. best 10.46
EC50 4 meas. best 10.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Somatostatin receptor type 2
CHEMBL1804
 Ki 10.46 10.0414 0.0 7
Somatostatin receptor type 5
CHEMBL1792
 EC50 10.19 9.955 0.1 2
Unchecked
CHEMBL612545
 IC50 10.13 9.752 0.1 5
Somatostatin receptor
CHEMBL2111427
 IC50 10.13 8.01 0.1 2
Somatostatin receptor type 4
CHEMBL1853
 IC50 10.1 9.044 0.1 5
Somatostatin receptor type 3
CHEMBL2238
 IC50 10.1 10.1 0.1 1
Somatostatin receptor type 2
CHEMBL1804
 EC50 10.0 10.0 0.1 1
Rattus norvegicus
CHEMBL376
 IC50 10.0 9.66 0.1 3
Somatostatin receptor type 3
CHEMBL2028
 Ki 10.0 9.4733 0.1 6
Somatostatin receptor type 5
CHEMBL1792
 Ki 9.92 9.421 0.1 10
Unchecked
CHEMBL612545
 Ki 9.89 9.8033 0.1 3
Somatostatin receptor type 1
CHEMBL1917
 IC50 9.85 9.0225 0.1 4
Somatostatin receptor
CHEMBL2096977
 IC50 9.7 9.535 0.2 2
Somatostatin receptor type 5
CHEMBL1792
 IC50 9.7 8.704 0.2 5
Somatostatin receptor type 2
CHEMBL3207
 IC50 9.55 9.55 0.3 1
Somatostatin receptor type 1
CHEMBL1917
 Ki 9.54 9.2683 0.3 6
Somatostatin receptor type 3
CHEMBL2028
 IC50 9.4 8.7175 0.4 4
Somatostatin receptor type 2
CHEMBL1804
 IC50 9.4 9.2175 0.4 4
Somatostatin receptor type 4
CHEMBL1853
 Ki 9.23 8.9757 0.6 7
Somatostatin receptor type 3
CHEMBL2028
 EC50 9.11 9.11 0.8 1
Somatostatin receptor
CHEMBL2111436
 IC50 9.08 9.08 0.8 2
Somatostatin receptor type 5
CHEMBL4318
 IC50 9.07 9.07 0.9 1
Mu-type opioid receptor
CHEMBL270
 IC50 8.22 8.22 6.0 1
Delta-type opioid receptor
CHEMBL269
 IC50 5.7 5.7 2000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.03333 hr Not specified
T1/2 13.0 hr -
T1/2 0.05 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Somatostatin receptor type 2 Ki = 0.035 nM 10.46 Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cell... 11520208
Somatostatin receptor type 2 Ki = 0.04 nM 10.4 Binding affinity towards Somatostatin receptor type 2 (hsst2) 12477342
Somatostatin receptor type 2 Ki = 0.049 nM 10.31 Inhibition of human sst2 receptor expressed in CHO cells 11327607
Somatostatin receptor type 5 EC50 = 0.065 nM 10.19 Effective concentration on human somatostatin receptor 5 11266182
Somatostatin receptor IC50 = 0.074 nM 10.13 Displacement of [125I]Tyr11-somatostatin-14 from somatostatin receptor in mouse ... 26988801
Unchecked IC50 = 0.074 nM 10.13 Displacement of [125I]Tyr11-somatostatin-14 from Sst receptor in mouse AtT-20 ce... 27876250
Somatostatin receptor type 3 IC50 = 0.08 nM 10.1 Tested for inhibition of radioligand binding to cloned somatostatin receptor mSS... 9216843
Somatostatin receptor type 4 IC50 = 0.08 nM 10.1 Tested for inhibition of radioligand binding to cloned somatostatin receptor hSS... 9216843
Somatostatin receptor type 2 Ki = 0.083 nM 10.08 Inhibitory constant against human sst2 receptor at a dose of 10 uM 15982879
Somatostatin receptor type 2 EC50 = 0.1 nM 10.0 Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing hum... 15982879
Rattus norvegicus IC50 = 0.1 nM 10.0 Inhibitory concentration on GH release from rat pituitary cells 16220980
Somatostatin receptor type 3 Ki = 0.1 nM 10.0 Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cell... 11520208
Unchecked IC50 = 0.12 nM 9.92 Inhibition of somatostatin receptor 18588282
Somatostatin receptor type 5 Ki = 0.12 nM 9.92 Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cell... 11520208
Unchecked Ki = 0.13 nM 9.89 Displacement of radiolabeled somatostatin-14 from somatostatin receptor 18983139
Somatostatin receptor type 3 Ki = 0.14 nM 9.85 Inhibition of human sst3 receptor expressed in CHO cells 11327607
Somatostatin receptor type 1 IC50 = 0.14 nM 9.85 Binding affinity to Somatostatin receptor type 1 (unknown origin) by radioligand... 23582449
Somatostatin receptor type 5 Ki = 0.14 nM 9.85 Inhibition of human sst5 receptor expressed in CHO cells 11327607
Somatostatin receptor type 5 Ki = 0.15 nM 9.82 Binding affinity against human sst5 receptor at a dose of 10 uM 15982879
Unchecked Ki = 0.15 nM 9.82 Binding affinity to SST (unknown origin) assessed as inhibition constant 28849908

Literature References

PubMed DOI Target Context # Activities
15982879 10.1016/j.bmcl.2005.05.061 Somatostatin receptor type 5 5
16220980 10.1021/jm050376t Rattus norvegicus 4
15658865 10.1021/jm049519m Rattus norvegicus 3
21806016 10.1021/jm200307v Somatostatin receptor type 3 3
35420805 10.1021/acs.jmedchem.2c00094 ADMET 2
11266182 10.1016/s0960-894x(01)00051-8 Somatostatin receptor type 5 2
18983139 10.1021/jm8007618 Unchecked 2
16220980 10.1021/jm050376t Somatostatin receptor type 5 2
16134928 10.1021/jm050524f Somatostatin receptor 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
16220980 10.1021/jm050376t Somatostatin receptor type 2 2
15982879 10.1016/j.bmcl.2005.05.061 Somatostatin receptor type 2 2
23466604 10.1016/j.ejmech.2013.01.044 Unchecked 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
16220980 10.1021/jm050376t Somatostatin receptor type 3 2
28849908 10.1021/acschembio.7b00481 Unchecked 2
15358539 10.1016/j.febslet.2004.07.084 ATP-dependent translocase ABCB1 2
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 2
9216843 10.1021/jm960850i Somatostatin receptor type 4 1
9216843 10.1021/jm960850i Somatostatin receptor type 5 1

Data from ChEMBL 36 via Core Engine