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Assay Detail

CHEMBL888113

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

Binding
Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane
ChEMBL ↗
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Somatostatin receptor type 1 (CHEMBL4652) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
Hurth K, Enz A, Floersheim P, Gentsch C, Hoyer D, Langenegger D, Neumann P, Pfäffli P, Sorg D, Swoboda R, Vassout A, Troxler T.
Bioorg Med Chem Lett (2007) 17 : 3988 -3991
PubMed 17512199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 55 7.32 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251541 OBELIN — 1 9.15
CHEMBL248715 — — 1 8.91
CHEMBL398681 — — 1 8.89
CHEMBL250498 — — 1 8.88
CHEMBL250922 — — 1 8.77
CHEMBL400137 — — 1 8.76
CHEMBL249930 — — 1 8.70
CHEMBL251120 — — 1 8.56
CHEMBL250304 — — 1 8.55
CHEMBL400136 — — 1 8.55
CHEMBL250305 — — 1 8.49
CHEMBL249723 — — 1 8.48
CHEMBL400907 — — 1 8.47
CHEMBL440233 — — 1 8.45
CHEMBL250921 — — 1 8.44
CHEMBL398656 — — 1 8.24
CHEMBL440235 — — 1 8.14
CHEMBL398655 — — 1 8.12
CHEMBL249932 — — 1 8.09
CHEMBL250522 — — 1 8.06
CHEMBL400099 — — 1 7.97
CHEMBL251334 — — 1 7.76
CHEMBL251311 — — 1 7.75
CHEMBL400709 — — 1 7.63
CHEMBL250724 — — 1 7.56
CHEMBL250914 — — 1 7.52
CHEMBL5483015 ARSENIC TRIOXIDE 4.0 1 7.28
CHEMBL251300 — — 1 7.15
CHEMBL250912 — — 1 7.09
CHEMBL250521 — — 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251541 OBELIN Kd = 0.7079 nM 9.15
CHEMBL248715 — Kd = 1.23 nM 8.91
CHEMBL398681 — Kd = 1.288 nM 8.89
CHEMBL250498 — Kd = 1.318 nM 8.88
CHEMBL250922 — Kd = 1.698 nM 8.77
CHEMBL400137 — Kd = 1.738 nM 8.76
CHEMBL249930 — Kd = 1.995 nM 8.70
CHEMBL251120 — Kd = 2.754 nM 8.56
CHEMBL250304 — Kd = 2.818 nM 8.55
CHEMBL400136 — Kd = 2.818 nM 8.55
CHEMBL250305 — Kd = 3.236 nM 8.49
CHEMBL249723 — Kd = 3.311 nM 8.48
CHEMBL400907 — Kd = 3.388 nM 8.47
CHEMBL440233 — Kd = 3.548 nM 8.45
CHEMBL250921 — Kd = 3.631 nM 8.44
CHEMBL398656 — Kd = 5.754 nM 8.24
CHEMBL440235 — Kd = 7.244 nM 8.14
CHEMBL398655 — Kd = 7.586 nM 8.12
CHEMBL249932 — Kd = 8.128 nM 8.09
CHEMBL250522 — Kd = 8.71 nM 8.06
CHEMBL400099 — Kd = 10.72 nM 7.97
CHEMBL251334 — Kd = 17.38 nM 7.76
CHEMBL251311 — Kd = 17.78 nM 7.75
CHEMBL400709 — Kd = 23.44 nM 7.63
CHEMBL250724 — Kd = 27.54 nM 7.56
CHEMBL250914 — Kd = 30.2 nM 7.52
CHEMBL5483015 ARSENIC TRIOXIDE Kd = 52.48 nM 7.28
CHEMBL251300 — Kd = 70.79 nM 7.15
CHEMBL250912 — Kd = 81.28 nM 7.09
CHEMBL250521 — Kd = 87.1 nM 7.06
CHEMBL251121 — Kd = 87.1 nM 7.06
CHEMBL251116 — Kd = 104.71 nM 6.98
CHEMBL250313 — Kd = 104.71 nM 6.98
CHEMBL428583 — Kd = 109.65 nM 6.96
CHEMBL250705 — Kd = 151.36 nM 6.82
CHEMBL250900 — Kd = 162.18 nM 6.79
CHEMBL250713 — Kd = 208.93 nM 6.68
CHEMBL250715 — Kd = 263.03 nM 6.58
CHEMBL250703 — Kd = 275.42 nM 6.56
CHEMBL440962 — Kd = 288.4 nM 6.54
CHEMBL250920 — Kd = 354.81 nM 6.45
CHEMBL400386 — Kd = 457.09 nM 6.34
CHEMBL400677 — Kd = 467.74 nM 6.33
CHEMBL251110 — Kd = 489.78 nM 6.31
CHEMBL251111 — Kd = 489.78 nM 6.31
CHEMBL250314 — Kd = 562.34 nM 6.25
CHEMBL398319 — Kd = 588.84 nM 6.23
CHEMBL250098 — Kd = 630.96 nM 6.20
CHEMBL250704 — Kd = 630.96 nM 6.20
CHEMBL250723 — Kd = 691.83 nM 6.16