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Assay Detail

CHEMBL964159

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Binding
Binding affinity to rat sst2 receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.
Troxler T, Hurth K, Mattes H, Prashad M, Schoeffter P, Langenegger D, Enz A, Hoyer D.
Bioorg Med Chem Lett (2009) 19 : 1305 -1309
PubMed 19208473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 18 5.19 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514027 1 6.04
CHEMBL515907 1 5.74
CHEMBL516837 1 5.46
CHEMBL474345 1 5.39
CHEMBL523814 1 5.38
CHEMBL517921 1 5.29
CHEMBL462335 1 5.22
CHEMBL460542 1 5.19
CHEMBL462336 1 5.17
CHEMBL461988 1 5.16
CHEMBL470331 1 5.16
CHEMBL540705 1 5.09
CHEMBL474752 1 5.08
CHEMBL462158 1 5.06
CHEMBL462157 1 4.84
CHEMBL460934 1 4.78
CHEMBL462159 1 4.73
CHEMBL473763 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514027 Kd = 912.01 nM 6.04
CHEMBL515907 Kd = 1819.7 nM 5.74
CHEMBL516837 Kd = 3467.37 nM 5.46
CHEMBL474345 Kd = 4073.8 nM 5.39
CHEMBL523814 Kd = 4168.69 nM 5.38
CHEMBL517921 Kd = 5128.61 nM 5.29
CHEMBL462335 Kd = 6025.6 nM 5.22
CHEMBL460542 Kd = 6456.54 nM 5.19
CHEMBL462336 Kd = 6760.83 nM 5.17
CHEMBL461988 Kd = 6918.31 nM 5.16
CHEMBL470331 Kd = 6918.31 nM 5.16
CHEMBL540705 Kd = 8128.31 nM 5.09
CHEMBL474752 Kd = 8317.64 nM 5.08
CHEMBL462158 Kd = 8709.64 nM 5.06
CHEMBL462157 Kd = 14454.4 nM 4.84
CHEMBL460934 Kd = 16595.87 nM 4.78
CHEMBL462159 Kd = 18620.87 nM 4.73
CHEMBL473763 Kd = 19498.45 nM 4.71