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Assay Detail

CHEMBL3373238

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

Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
McCoull W, Barton P, Brown AJ, Bowker SS, Cameron J, Clarke DS, Davies RD, Dossetter AG, Ertan A, Fenwick M, Green C, Holmes JL, Martin N, Masters D, Moore JE, Newcombe NJ, Newton C, Pointon H, Robb GR, Sheldon C, Stokes S, Morgan D.
J Med Chem (2014) 57 : 6128 -6140
PubMed 24967667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 8.45 10.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319217 1 10.11
CHEMBL3319221 1 9.82
CHEMBL3319398 1 9.62
CHEMBL3319222 1 9.54
CHEMBL3319220 1 9.51
CHEMBL3319397 1 9.51
CHEMBL3319219 1 9.48
CHEMBL3319407 1 9.40
CHEMBL3319400 1 9.37
CHEMBL3319228 1 9.32
CHEMBL3319227 1 9.28
CHEMBL3319399 1 9.24
CHEMBL3319396 1 9.21
CHEMBL3319225 1 9.17
CHEMBL3319224 1 9.16
CHEMBL3319223 1 9.11
CHEMBL3319406 1 9.04
CHEMBL3319229 1 8.89
CHEMBL3319215 1 8.89
CHEMBL3319402 1 8.54
CHEMBL3319401 1 8.41
CHEMBL3319216 1 8.38
CHEMBL3319218 1 8.29
CHEMBL3319405 1 8.17
CHEMBL3319408 1 8.14
CHEMBL3319214 1 8.07
CHEMBL3319211 1 8.06
CHEMBL3319226 1 8.06
CHEMBL3319212 1 7.89
CHEMBL3319403 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319217 IC50 = 0.078 nM 10.11
CHEMBL3319221 IC50 = 0.15 nM 9.82
CHEMBL3319398 IC50 = 0.24 nM 9.62
CHEMBL3319222 IC50 = 0.29 nM 9.54
CHEMBL3319220 IC50 = 0.31 nM 9.51
CHEMBL3319397 IC50 = 0.31 nM 9.51
CHEMBL3319219 IC50 = 0.33 nM 9.48
CHEMBL3319407 IC50 = 0.4 nM 9.40
CHEMBL3319400 IC50 = 0.43 nM 9.37
CHEMBL3319228 IC50 = 0.48 nM 9.32
CHEMBL3319227 IC50 = 0.53 nM 9.28
CHEMBL3319399 IC50 = 0.57 nM 9.24
CHEMBL3319396 IC50 = 0.62 nM 9.21
CHEMBL3319225 IC50 = 0.67 nM 9.17
CHEMBL3319224 IC50 = 0.69 nM 9.16
CHEMBL3319223 IC50 = 0.77 nM 9.11
CHEMBL3319406 IC50 = 0.92 nM 9.04
CHEMBL3319229 IC50 = 1.3 nM 8.89
CHEMBL3319215 IC50 = 1.3 nM 8.89
CHEMBL3319402 IC50 = 2.9 nM 8.54
CHEMBL3319401 IC50 = 3.9 nM 8.41
CHEMBL3319216 IC50 = 4.2 nM 8.38
CHEMBL3319218 IC50 = 5.1 nM 8.29
CHEMBL3319405 IC50 = 6.7 nM 8.17
CHEMBL3319408 IC50 = 7.2 nM 8.14
CHEMBL3319214 IC50 = 8.6 nM 8.07
CHEMBL3319211 IC50 = 8.7 nM 8.06
CHEMBL3319226 IC50 = 8.8 nM 8.06
CHEMBL3319212 IC50 = 13.0 nM 7.89
CHEMBL3319403 IC50 = 15.0 nM 7.82
CHEMBL3319282 IC50 = 23.0 nM 7.64
CHEMBL3319280 IC50 = 27.0 nM 7.57
CHEMBL3319404 IC50 = 33.0 nM 7.48
CHEMBL3319279 IC50 = 44.0 nM 7.36
CHEMBL3319213 IC50 = 65.0 nM 7.19
CHEMBL3319275 IC50 = 76.0 nM 7.12
CHEMBL3319281 IC50 = 83.0 nM 7.08
CHEMBL3319276 IC50 = 120.0 nM 6.92
CHEMBL3319274 IC50 = 210.0 nM 6.68
CHEMBL3319277 IC50 = 4700.0 nM 5.33
CHEMBL3319278 IC50 > 10000.0 nM -