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Assay Detail

CHEMBL888089

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

Binding
Displacement of [125I]SRIF14 from sst2 receptor in rat brain cortex membrane
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Somatostatin receptor type 2 (CHEMBL2978)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification and SAR of potent and selective non-peptide obeline somatostatin sst1 receptor antagonists.
Troxler T, Hoyer D, Langenegger D, Neumann P, Pfäffli P, Schoeffter P, Sorg D, Swoboda R, Hurth K.
Bioorg Med Chem Lett (2007) 17 : 3983 -3987
PubMed 17507221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 25 5.12 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251753 1 5.72
CHEMBL249111 1 5.54
CHEMBL399843 1 5.45
CHEMBL440236 1 5.43
CHEMBL251754 1 5.41
CHEMBL399464 1 5.32
CHEMBL401290 1 5.29
CHEMBL248715 1 5.24
CHEMBL251542 1 5.24
CHEMBL248907 1 5.20
CHEMBL251752 1 5.14
CHEMBL401091 1 5.14
CHEMBL251543 1 5.11
CHEMBL251541 OBELIN 1 5.11
CHEMBL248716 1 5.04
CHEMBL248717 1 5.00
CHEMBL248908 1 5.00
CHEMBL249113 1 4.99
CHEMBL251334 1 4.99
CHEMBL399658 1 4.96
CHEMBL399267 1 4.86
CHEMBL249112 1 4.83
CHEMBL251751 1 4.81
CHEMBL251529 1 4.78
CHEMBL251335 1 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251753 Kd = 1905.46 nM 5.72
CHEMBL249111 Kd = 2884.03 nM 5.54
CHEMBL399843 Kd = 3548.13 nM 5.45
CHEMBL440236 Kd = 3715.35 nM 5.43
CHEMBL251754 Kd = 3890.45 nM 5.41
CHEMBL399464 Kd = 4786.3 nM 5.32
CHEMBL401290 Kd = 5128.61 nM 5.29
CHEMBL248715 Kd = 5754.4 nM 5.24
CHEMBL251542 Kd = 5754.4 nM 5.24
CHEMBL248907 Kd = 6309.57 nM 5.20
CHEMBL251752 Kd = 7244.36 nM 5.14
CHEMBL401091 Kd = 7244.36 nM 5.14
CHEMBL251543 Kd = 7762.47 nM 5.11
CHEMBL251541 OBELIN Kd = 7762.47 nM 5.11
CHEMBL248716 Kd = 9120.11 nM 5.04
CHEMBL248717 Kd = 10000.0 nM 5.00
CHEMBL248908 Kd = 10000.0 nM 5.00
CHEMBL249113 Kd = 10232.93 nM 4.99
CHEMBL251334 Kd = 10232.93 nM 4.99
CHEMBL399658 Kd = 10964.78 nM 4.96
CHEMBL399267 Kd = 13803.84 nM 4.86
CHEMBL249112 Kd = 14791.08 nM 4.83
CHEMBL251751 Kd = 15488.17 nM 4.81
CHEMBL251529 Kd = 16595.87 nM 4.78
CHEMBL251335 Kd = 32359.37 nM 4.49