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Assay Detail

CHEMBL3620280

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

Binding
Displacement of [125I]-GLP1 from human GLP1 receptor expressed in BHK cells after 2 hrs in presence of 2% human serum albumin
48
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucagon-like peptide 1 receptor (CHEMBL1784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.
Lau J, Bloch P, Schäffer L, Pettersson I, Spetzler J, Kofoed J, Madsen K, Knudsen LB, McGuire J, Steensgaard DB, Strauss HM, Gram DX, Knudsen SM, Nielsen FS, Thygesen P, Reedtz-Runge S, Kruse T.
J Med Chem (2015) 58 : 7370 -7380
PubMed 26308095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 8.05 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3616718 1 10.10
CHEMBL428139 1 10.00
CHEMBL3616711 1 9.85
CHEMBL3616742 1 9.66
CHEMBL3616740 1 9.12
CHEMBL3616744 1 9.06
CHEMBL3616713 1 9.01
CHEMBL3616712 1 8.71
CHEMBL3616743 1 8.70
CHEMBL3616741 1 8.47
CHEMBL3616717 1 8.42
CHEMBL3616771 1 8.40
CHEMBL4084119 LIRAGLUTIDE 4.0 1 8.32
CHEMBL3616745 1 8.32
CHEMBL3616739 1 8.30
CHEMBL3616764 1 8.27
CHEMBL3616754 1 8.21
CHEMBL3616774 1 8.19
CHEMBL3616773 1 8.17
CHEMBL3616770 1 8.12
CHEMBL3616762 1 8.07
CHEMBL3616759 1 8.06
CHEMBL3616746 1 8.05
CHEMBL3616755 1 7.94
CHEMBL3616753 1 7.89
CHEMBL3616747 1 7.89
CHEMBL3616480 1 7.84
CHEMBL3616757 1 7.82
CHEMBL3616758 1 7.78
CHEMBL3616767 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3616718 IC50 = 0.08 nM 10.10
CHEMBL428139 IC50 = 0.1 nM 10.00
CHEMBL3616711 IC50 = 0.14 nM 9.85
CHEMBL3616742 IC50 = 0.22 nM 9.66
CHEMBL3616740 IC50 = 0.75 nM 9.12
CHEMBL3616744 IC50 = 0.88 nM 9.06
CHEMBL3616713 IC50 = 0.97 nM 9.01
CHEMBL3616712 IC50 = 1.95 nM 8.71
CHEMBL3616743 IC50 = 1.99 nM 8.70
CHEMBL3616741 IC50 = 3.4 nM 8.47
CHEMBL3616717 IC50 = 3.78 nM 8.42
CHEMBL3616771 IC50 = 3.99 nM 8.40
CHEMBL3616745 IC50 = 4.75 nM 8.32
CHEMBL4084119 LIRAGLUTIDE IC50 = 4.78 nM 8.32
CHEMBL3616739 IC50 = 5.05 nM 8.30
CHEMBL3616764 IC50 = 5.39 nM 8.27
CHEMBL3616754 IC50 = 6.17 nM 8.21
CHEMBL3616774 IC50 = 6.5 nM 8.19
CHEMBL3616773 IC50 = 6.73 nM 8.17
CHEMBL3616770 IC50 = 7.55 nM 8.12
CHEMBL3616762 IC50 = 8.43 nM 8.07
CHEMBL3616759 IC50 = 8.8 nM 8.06
CHEMBL3616746 IC50 = 8.87 nM 8.05
CHEMBL3616755 IC50 = 11.4 nM 7.94
CHEMBL3616753 IC50 = 12.9 nM 7.89
CHEMBL3616747 IC50 = 12.8 nM 7.89
CHEMBL3616480 IC50 = 14.5 nM 7.84
CHEMBL3616757 IC50 = 15.2 nM 7.82
CHEMBL3616758 IC50 = 16.8 nM 7.78
CHEMBL3616767 IC50 = 17.7 nM 7.75
CHEMBL3616766 IC50 = 19.3 nM 7.71
CHEMBL3616756 IC50 = 19.5 nM 7.71
CHEMBL3616748 IC50 = 20.5 nM 7.69
CHEMBL3616760 IC50 = 20.7 nM 7.68
CHEMBL3616769 IC50 = 23.0 nM 7.64
CHEMBL3616763 IC50 = 24.8 nM 7.61
CHEMBL3616765 IC50 = 25.5 nM 7.59
CHEMBL3616749 IC50 = 27.0 nM 7.57
CHEMBL2108724 SEMAGLUTIDE IC50 = 30.0 nM 7.52
CHEMBL3616772 IC50 = 30.1 nM 7.52
CHEMBL3616768 IC50 = 41.6 nM 7.38
CHEMBL3616761 IC50 = 51.7 nM 7.29
CHEMBL3616714 IC50 = 74.0 nM 7.13
CHEMBL3616751 IC50 = 79.7 nM 7.10
CHEMBL3616750 IC50 = 112.0 nM 6.95
CHEMBL3616716 IC50 = 148.0 nM 6.83
CHEMBL3616715 IC50 = 295.0 nM 6.53
CHEMBL2108724 SEMAGLUTIDE IC50 = 357.0 nM 6.45