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Assay Detail

CHEMBL805715

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro binding affinity at somatostatin 2 receptor in transfected HEK 293 cell using [125 I]Tyr11-SRIF-14 as radioligand
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Somatostatin receptor type 2 (CHEMBL1804)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas.
Liu S, Tang C, Ho B, Ankersen M, Stidsen CE, Crider AM.
J Med Chem (1998) 41 : 4693 -4705
PubMed 9822540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.13 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823872 SOMATOSTATIN 3.0 1 9.70
CHEMBL3350037 1 9.52
CHEMBL311695 SEGLITIDE 2.0 1 9.52
CHEMBL140151 1 6.51
CHEMBL344404 1 6.30
CHEMBL433872 1 6.25
CHEMBL103769 1 6.21
CHEMBL142986 1 6.11
CHEMBL359215 1 6.11
CHEMBL145472 1 6.08
CHEMBL142422 1 6.05
CHEMBL143668 1 6.00
CHEMBL142402 1 6.00
CHEMBL142283 1 5.80
CHEMBL142549 1 5.77
CHEMBL142613 1 5.77
CHEMBL344285 1 5.70
CHEMBL143409 1 5.70
CHEMBL143164 1 5.70
CHEMBL142823 1 5.66
CHEMBL142321 1 5.64
CHEMBL359453 1 5.60
CHEMBL344074 1 5.52
CHEMBL344059 1 5.38
CHEMBL143100 1 5.34
CHEMBL142492 1 5.10
CHEMBL142822 1 4.48
CHEMBL142295 1 4.13
CHEMBL142811 1 -
CHEMBL422475 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823872 SOMATOSTATIN Ki = 0.2 nM 9.70
CHEMBL3350037 Ki = 0.3 nM 9.52
CHEMBL311695 SEGLITIDE Ki = 0.3 nM 9.52
CHEMBL140151 Ki = 310.0 nM 6.51
CHEMBL344404 Ki = 500.0 nM 6.30
CHEMBL433872 Ki = 565.0 nM 6.25
CHEMBL103769 Ki = 621.0 nM 6.21
CHEMBL142986 Ki = 778.0 nM 6.11
CHEMBL359215 Ki = 777.0 nM 6.11
CHEMBL145472 Ki = 830.0 nM 6.08
CHEMBL142422 Ki = 894.0 nM 6.05
CHEMBL143668 Ki = 1000.0 nM 6.00
CHEMBL142402 Ki = 1000.0 nM 6.00
CHEMBL142283 Ki = 1600.0 nM 5.80
CHEMBL142613 Ki = 1700.0 nM 5.77
CHEMBL142549 Ki = 1700.0 nM 5.77
CHEMBL143164 Ki = 2000.0 nM 5.70
CHEMBL143409 Ki = 2000.0 nM 5.70
CHEMBL344285 Ki = 2000.0 nM 5.70
CHEMBL142823 Ki = 2200.0 nM 5.66
CHEMBL142321 Ki = 2300.0 nM 5.64
CHEMBL359453 Ki = 2500.0 nM 5.60
CHEMBL344074 Ki = 3000.0 nM 5.52
CHEMBL344059 Ki = 4200.0 nM 5.38
CHEMBL143100 Ki = 4600.0 nM 5.34
CHEMBL142492 Ki = 8000.0 nM 5.10
CHEMBL142822 Ki = 33000.0 nM 4.48
CHEMBL142295 Ki = 74000.0 nM 4.13
CHEMBL142811 Ki > 300000.0 nM -
CHEMBL422475 Ki = 114000.0 nM -
CHEMBL342781 Ki > 300000.0 nM -
CHEMBL143245 Ki > 300000.0 nM -
CHEMBL143539 Ki > 300000.0 nM -
CHEMBL142293 Ki > 300000.0 nM -