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Assay Detail

CHEMBL1102012

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

Binding
Binding affinity to human SST1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Somatostatin receptor type 1 (CHEMBL1917)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst(3) receptor antagonists.
Troxler T, Hurth K, Schuh KH, Schoeffter P, Langenegger D, Enz A, Hoyer D.
Bioorg Med Chem Lett (2010) 20 : 1728 -1734
PubMed 20137944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 25 6.15 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461988 1 8.12
CHEMBL1076627 1 7.40
CHEMBL470331 1 7.11
CHEMBL1080734 1 6.99
CHEMBL1080733 1 6.92
CHEMBL1076659 1 6.40
CHEMBL1076620 1 6.36
CHEMBL1076652 1 6.31
CHEMBL1076654 1 6.27
CHEMBL1076625 1 6.14
CHEMBL1076717 1 6.04
CHEMBL1076655 1 6.04
CHEMBL1076621 1 6.03
CHEMBL1076657 1 6.00
CHEMBL1076622 1 5.86
CHEMBL1076623 1 5.81
CHEMBL1076718 1 5.79
CHEMBL1076711 1 5.72
CHEMBL1076624 1 5.69
CHEMBL1076710 1 5.63
CHEMBL1076658 1 5.63
CHEMBL1076653 1 5.61
CHEMBL1076709 1 5.58
CHEMBL1076656 1 5.21
CHEMBL1076719 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461988 Kd = 7.586 nM 8.12
CHEMBL1076627 Kd = 39.81 nM 7.40
CHEMBL470331 Kd = 77.62 nM 7.11
CHEMBL1080734 Kd = 102.33 nM 6.99
CHEMBL1080733 Kd = 120.23 nM 6.92
CHEMBL1076659 Kd = 398.11 nM 6.40
CHEMBL1076620 Kd = 436.52 nM 6.36
CHEMBL1076652 Kd = 489.78 nM 6.31
CHEMBL1076654 Kd = 537.03 nM 6.27
CHEMBL1076625 Kd = 724.44 nM 6.14
CHEMBL1076717 Kd = 912.01 nM 6.04
CHEMBL1076655 Kd = 912.01 nM 6.04
CHEMBL1076621 Kd = 933.25 nM 6.03
CHEMBL1076657 Kd = 1000.0 nM 6.00
CHEMBL1076622 Kd = 1380.38 nM 5.86
CHEMBL1076623 Kd = 1548.82 nM 5.81
CHEMBL1076718 Kd = 1621.81 nM 5.79
CHEMBL1076711 Kd = 1905.46 nM 5.72
CHEMBL1076624 Kd = 2041.74 nM 5.69
CHEMBL1076710 Kd = 2344.23 nM 5.63
CHEMBL1076658 Kd = 2344.23 nM 5.63
CHEMBL1076653 Kd = 2454.71 nM 5.61
CHEMBL1076709 Kd = 2630.27 nM 5.58
CHEMBL1076656 Kd = 6165.95 nM 5.21
CHEMBL1076719 Kd = 9120.11 nM 5.04