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Assay Detail

CHEMBL685178

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

Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Growth hormone secretagogue receptor type 1 (CHEMBL4616)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics.
Palucki BL, Feighner SD, Pong S, McKee KK, Hreniuk DL, Tan C, Howard AD, Van der Ploeg LH, Patchett AA, Nargund RP.
Bioorg Med Chem Lett (2001) 11 : 1955 -1957
PubMed 11459669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.18 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL500468 GHRELIN 3.0 1 9.60
CHEMBL13817 IBUTAMOREN 2.0 1 9.20
CHEMBL294324 1 8.09
CHEMBL301259 1 7.44
CHEMBL61292 1 6.89
CHEMBL294408 1 6.68
CHEMBL59572 1 6.23
CHEMBL291333 1 6.08
CHEMBL61663 1 6.05
CHEMBL58758 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL500468 GHRELIN IC50 = 0.25 nM 9.60
CHEMBL13817 IBUTAMOREN IC50 = 0.63 nM 9.20
CHEMBL294324 IC50 = 8.12 nM 8.09
CHEMBL301259 IC50 = 36.2 nM 7.44
CHEMBL61292 IC50 = 128.0 nM 6.89
CHEMBL294408 IC50 = 209.0 nM 6.68
CHEMBL59572 IC50 = 590.5 nM 6.23
CHEMBL291333 IC50 = 828.5 nM 6.08
CHEMBL61663 IC50 = 889.0 nM 6.05
CHEMBL58758 IC50 = 2670.0 nM 5.57