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Assay Detail

CHEMBL3620282

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Functional
Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin
ChEMBL ↗
48
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 48 10.35 10.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3616760 — — 1 10.97
CHEMBL3616740 — — 1 10.95
CHEMBL3616762 — — 1 10.94
CHEMBL3616771 — — 1 10.88
CHEMBL3616741 — — 1 10.83
CHEMBL3616746 — — 1 10.80
CHEMBL428139 — — 1 10.79
CHEMBL3616712 — — 1 10.77
CHEMBL3616739 — — 1 10.72
CHEMBL3616759 — — 1 10.67
CHEMBL3616763 — — 1 10.61
CHEMBL3616774 — — 1 10.59
CHEMBL3616756 — — 1 10.56
CHEMBL3616754 — — 1 10.56
CHEMBL3616766 — — 1 10.39
CHEMBL3616768 — — 1 10.38
CHEMBL3616745 — — 1 10.37
CHEMBL3616755 — — 1 10.33
CHEMBL3616773 — — 1 10.17
CHEMBL3616757 — — 1 10.17
CHEMBL3616714 — — 1 10.15
CHEMBL3616758 — — 1 10.15
CHEMBL3616770 — — 1 10.06
CHEMBL3616769 — — 1 9.80
CHEMBL3616747 — — 1 9.78
CHEMBL3616715 — — 1 9.62
CHEMBL3616749 — — 1 9.57
CHEMBL3616761 — — 1 8.22
CHEMBL3616480 — — 1 -
CHEMBL3616764 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3616760 — EC50 = 0.0107 nM 10.97
CHEMBL3616740 — EC50 = 0.0111 nM 10.95
CHEMBL3616762 — EC50 = 0.0115 nM 10.94
CHEMBL3616771 — EC50 = 0.0132 nM 10.88
CHEMBL3616741 — EC50 = 0.0147 nM 10.83
CHEMBL3616746 — EC50 = 0.0157 nM 10.80
CHEMBL428139 — EC50 = 0.0162 nM 10.79
CHEMBL3616712 — EC50 = 0.0171 nM 10.77
CHEMBL3616739 — EC50 = 0.0192 nM 10.72
CHEMBL3616759 — EC50 = 0.0212 nM 10.67
CHEMBL3616763 — EC50 = 0.0244 nM 10.61
CHEMBL3616774 — EC50 = 0.026 nM 10.59
CHEMBL3616754 — EC50 = 0.0277 nM 10.56
CHEMBL3616756 — EC50 = 0.0278 nM 10.56
CHEMBL3616766 — EC50 = 0.0409 nM 10.39
CHEMBL3616768 — EC50 = 0.0418 nM 10.38
CHEMBL3616745 — EC50 = 0.0426 nM 10.37
CHEMBL3616755 — EC50 = 0.0473 nM 10.33
CHEMBL3616773 — EC50 = 0.0675 nM 10.17
CHEMBL3616757 — EC50 = 0.067 nM 10.17
CHEMBL3616758 — EC50 = 0.0703 nM 10.15
CHEMBL3616714 — EC50 = 0.0709 nM 10.15
CHEMBL3616770 — EC50 = 0.0873 nM 10.06
CHEMBL3616769 — EC50 = 0.159 nM 9.80
CHEMBL3616747 — EC50 = 0.166 nM 9.78
CHEMBL3616715 — EC50 = 0.238 nM 9.62
CHEMBL3616749 — EC50 = 0.269 nM 9.57
CHEMBL3616761 — EC50 = 5.99 nM 8.22
CHEMBL3616711 — EC50 = 0.0076 nM -
CHEMBL4084119 LIRAGLUTIDE EC50 = 0.0085 nM -
CHEMBL3616713 — EC50 = 0.0037 nM -
CHEMBL3616716 — EC50 = 0.0038 nM -
CHEMBL3616718 — EC50 = 0.0062 nM -
CHEMBL3616717 — EC50 = 0.0027 nM -
CHEMBL3616742 — EC50 = 0.0043 nM -
CHEMBL3616743 — EC50 = 0.0032 nM -
CHEMBL3616744 — EC50 = 0.0048 nM -
CHEMBL3616748 — EC50 = 0.0086 nM -
CHEMBL3616750 — EC50 = 0.0099 nM -
CHEMBL3616751 — EC50 = 0.0048 nM -
CHEMBL2108724 SEMAGLUTIDE EC50 = 0.0062 nM -
CHEMBL3616753 — EC50 = 0.0056 nM -
CHEMBL2108724 SEMAGLUTIDE EC50 = 0.0071 nM -
CHEMBL3616767 — EC50 = 0.0027 nM -
CHEMBL3616765 — EC50 = 0.0099 nM -
CHEMBL3616764 — EC50 = 0.0046 nM -
CHEMBL3616480 — EC50 = 0.007 nM -
CHEMBL3616772 — EC50 = 0.0015 nM -