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Assay Detail

CHEMBL888088

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

Binding
Displacement of [125I]SRIF14 from sst1 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 1 (CHEMBL4652)
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 8.43 9.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401290 1 9.67
CHEMBL251754 1 9.40
CHEMBL440236 1 9.39
CHEMBL251753 1 9.24
CHEMBL251541 OBELIN 1 9.15
CHEMBL251542 1 9.09
CHEMBL248908 1 9.08
CHEMBL248907 1 8.92
CHEMBL249113 1 8.92
CHEMBL399464 1 8.92
CHEMBL248715 1 8.91
CHEMBL399658 1 8.85
CHEMBL399843 1 8.81
CHEMBL399267 1 8.45
CHEMBL248716 1 8.34
CHEMBL251751 1 8.32
CHEMBL251752 1 8.22
CHEMBL248717 1 8.10
CHEMBL401091 1 7.80
CHEMBL251334 1 7.76
CHEMBL251543 1 7.73
CHEMBL251529 1 7.60
CHEMBL249111 1 7.46
CHEMBL251335 1 6.80
CHEMBL249112 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401290 Kd = 0.2138 nM 9.67
CHEMBL251754 Kd = 0.3981 nM 9.40
CHEMBL440236 Kd = 0.4074 nM 9.39
CHEMBL251753 Kd = 0.5754 nM 9.24
CHEMBL251541 OBELIN Kd = 0.7079 nM 9.15
CHEMBL251542 Kd = 0.8128 nM 9.09
CHEMBL248908 Kd = 0.8318 nM 9.08
CHEMBL248907 Kd = 1.202 nM 8.92
CHEMBL249113 Kd = 1.202 nM 8.92
CHEMBL399464 Kd = 1.202 nM 8.92
CHEMBL248715 Kd = 1.23 nM 8.91
CHEMBL399658 Kd = 1.413 nM 8.85
CHEMBL399843 Kd = 1.549 nM 8.81
CHEMBL399267 Kd = 3.548 nM 8.45
CHEMBL248716 Kd = 4.571 nM 8.34
CHEMBL251751 Kd = 4.786 nM 8.32
CHEMBL251752 Kd = 6.026 nM 8.22
CHEMBL248717 Kd = 7.943 nM 8.10
CHEMBL401091 Kd = 15.85 nM 7.80
CHEMBL251334 Kd = 17.38 nM 7.76
CHEMBL251543 Kd = 18.62 nM 7.73
CHEMBL251529 Kd = 25.12 nM 7.60
CHEMBL249111 Kd = 34.67 nM 7.46
CHEMBL251335 Kd = 158.49 nM 6.80
CHEMBL249112 Kd = 1318.26 nM 5.88