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Assay Detail

CHEMBL5137205

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

Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Somatostatin receptor type 4 (CHEMBL1853)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of 3,4,5-trisubstituted-1,2,4-triazoles: high affinity and selective somatostatin receptor-4 agonists for Alzheimer's disease treatment.
Neumann WL, Sandoval KE, Mobayen S, Minaeian M, Kukielski SG, Srabony KN, Frare R, Slater O, Farr SA, Niehoff ML, Hospital A, Kontoyianni M, Crider AM, Witt KA.
RSC Med Chem (2021) 12 : 1352 -1365
PubMed 34458738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 59 8.10 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5174969 1 9.30
CHEMBL5183772 1 9.30
CHEMBL5197201 1 9.30
CHEMBL5185547 1 9.22
CHEMBL5179456 1 9.15
CHEMBL5175637 1 9.15
CHEMBL5172814 1 9.15
CHEMBL5193727 1 9.15
CHEMBL5180543 1 9.10
CHEMBL5177487 1 9.10
CHEMBL5209180 1 9.05
CHEMBL5177573 1 9.05
CHEMBL5190457 1 9.00
CHEMBL5171935 1 9.00
CHEMBL5176083 1 8.96
CHEMBL5190056 1 8.92
CHEMBL5180551 1 8.85
CHEMBL5173784 1 8.77
CHEMBL5188841 1 8.77
CHEMBL5208396 1 8.77
CHEMBL5206148 1 8.74
CHEMBL5193172 1 8.66
CHEMBL5205998 1 8.59
CHEMBL5195145 1 8.55
CHEMBL5196971 1 8.52
CHEMBL5178013 1 8.51
CHEMBL5200786 1 8.49
CHEMBL5198142 1 8.48
CHEMBL5193686 1 8.29
CHEMBL5205904 1 8.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5174969 Ki = 0.5 nM 9.30
CHEMBL5197201 Ki = 0.5 nM 9.30
CHEMBL5183772 Ki = 0.5 nM 9.30
CHEMBL5185547 Ki = 0.6 nM 9.22
CHEMBL5179456 Ki = 0.7 nM 9.15
CHEMBL5175637 Ki = 0.7 nM 9.15
CHEMBL5172814 Ki = 0.7 nM 9.15
CHEMBL5193727 Ki = 0.7 nM 9.15
CHEMBL5180543 Ki = 0.8 nM 9.10
CHEMBL5177487 Ki = 0.8 nM 9.10
CHEMBL5209180 Ki = 0.9 nM 9.05
CHEMBL5177573 Ki = 0.9 nM 9.05
CHEMBL5190457 Ki = 1.0 nM 9.00
CHEMBL5171935 Ki = 1.0 nM 9.00
CHEMBL5176083 Ki = 1.1 nM 8.96
CHEMBL5190056 Ki = 1.2 nM 8.92
CHEMBL5180551 Ki = 1.4 nM 8.85
CHEMBL5173784 Ki = 1.7 nM 8.77
CHEMBL5188841 Ki = 1.7 nM 8.77
CHEMBL5208396 Ki = 1.7 nM 8.77
CHEMBL5206148 Ki = 1.8 nM 8.74
CHEMBL5193172 Ki = 2.2 nM 8.66
CHEMBL5205998 Ki = 2.6 nM 8.59
CHEMBL5195145 Ki = 2.8 nM 8.55
CHEMBL5196971 Ki = 3.0 nM 8.52
CHEMBL5178013 Ki = 3.1 nM 8.51
CHEMBL5200786 Ki = 3.2 nM 8.49
CHEMBL5198142 Ki = 3.3 nM 8.48
CHEMBL5193686 Ki = 5.1 nM 8.29
CHEMBL5205904 Ki = 5.1 nM 8.29
CHEMBL5189042 Ki = 5.5 nM 8.26
CHEMBL5187631 Ki = 6.9 nM 8.16
CHEMBL5200112 Ki = 7.0 nM 8.15
CHEMBL5180752 Ki = 7.1 nM 8.15
CHEMBL5207543 Ki = 7.7 nM 8.11
CHEMBL5179321 Ki = 11.0 nM 7.96
CHEMBL5201594 Ki = 12.0 nM 7.92
CHEMBL5209165 Ki = 12.4 nM 7.91
CHEMBL5192791 Ki = 14.9 nM 7.83
CHEMBL5188361 Ki = 16.2 nM 7.79
CHEMBL5191532 Ki = 21.5 nM 7.67
CHEMBL5201540 Ki = 30.3 nM 7.52
CHEMBL5197218 Ki = 36.6 nM 7.44
CHEMBL5193951 Ki = 37.5 nM 7.43
CHEMBL5203972 Ki = 39.5 nM 7.40
CHEMBL5176020 Ki = 40.4 nM 7.39
CHEMBL5202717 Ki = 51.7 nM 7.29
CHEMBL5180116 Ki = 57.1 nM 7.24
CHEMBL5208764 Ki = 58.8 nM 7.23
CHEMBL5208037 Ki = 80.8 nM 7.09