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Assay Detail

CHEMBL3824477

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

Binding
Agonist activity at human GLP1R expressed in HEK293 cells after 5 hrs by luciferase reporter gene assay
85
Total Activities
85
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

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

Publication

Synthesis and Pharmacological Characterization of Novel Glucagon-like Peptide-2 (GLP-2) Analogues with Low Systemic Clearance.
Wiśniewski K, Sueiras-Diaz J, Jiang G, Galyean R, Lu M, Thompson D, Wang YC, Croston G, Posch A, Hargrove DM, Wiśniewska H, Laporte R, Dwyer JJ, Qi S, Srinivasan K, Hartwig J, Ferdyan N, Mares M, Kraus J, Alagarsamy S, Rivière PJ, Schteingart CD.
J Med Chem (2016) 59 : 3129 -3139
PubMed 26986178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 85 7.25 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4299664 1 8.06
CHEMBL3822701 1 8.05
CHEMBL4299677 1 8.00
CHEMBL3822593 1 7.80
CHEMBL4299655 1 7.68
CHEMBL3823755 1 7.50
CHEMBL3822625 1 7.41
CHEMBL3824159 1 7.40
CHEMBL3823411 1 7.35
CHEMBL3822981 1 7.25
CHEMBL3823448 1 7.22
CHEMBL3823334 1 7.16
CHEMBL3823889 1 7.10
CHEMBL3823221 1 7.08
CHEMBL3823421 1 7.05
CHEMBL3822975 1 7.00
CHEMBL3823878 1 6.96
CHEMBL3823876 1 6.92
CHEMBL3823835 1 6.89
CHEMBL3823333 1 6.75
CHEMBL3823760 1 6.52
CHEMBL2177395 1 6.28
CHEMBL3822636 1 -
CHEMBL4299631 1 -
CHEMBL3822928 1 -
CHEMBL3824278 1 -
CHEMBL3823643 1 -
CHEMBL4299662 1 -
CHEMBL3822459 1 -
CHEMBL3823976 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4299664 EC50 = 8.8 nM 8.06
CHEMBL3822701 EC50 = 8.9 nM 8.05
CHEMBL4299677 EC50 = 10.0 nM 8.00
CHEMBL3822593 EC50 = 16.0 nM 7.80
CHEMBL4299655 EC50 = 21.0 nM 7.68
CHEMBL3823755 EC50 = 32.0 nM 7.50
CHEMBL3822625 EC50 = 39.0 nM 7.41
CHEMBL3824159 EC50 = 40.0 nM 7.40
CHEMBL3823411 EC50 = 45.0 nM 7.35
CHEMBL3822981 EC50 = 56.0 nM 7.25
CHEMBL3823448 EC50 = 60.0 nM 7.22
CHEMBL3823334 EC50 = 70.0 nM 7.16
CHEMBL3823889 EC50 = 80.0 nM 7.10
CHEMBL3823221 EC50 = 83.0 nM 7.08
CHEMBL3823421 EC50 = 90.0 nM 7.05
CHEMBL3822975 EC50 = 100.0 nM 7.00
CHEMBL3823878 EC50 = 110.0 nM 6.96
CHEMBL3823876 EC50 = 120.0 nM 6.92
CHEMBL3823835 EC50 = 130.0 nM 6.89
CHEMBL3823333 EC50 = 180.0 nM 6.75
CHEMBL3823760 EC50 = 300.0 nM 6.52
CHEMBL2177395 EC50 = 520.0 nM 6.28
CHEMBL3824332 EC50 > 1000.0 nM -
CHEMBL3823043 EC50 > 1000.0 nM -
CHEMBL3824079 EC50 > 1000.0 nM -
CHEMBL3824232 EC50 > 1000.0 nM -
CHEMBL3823082 EC50 > 1000.0 nM -
CHEMBL3823541 EC50 > 1000.0 nM -
CHEMBL3823133 EC50 > 1000.0 nM -
CHEMBL3823291 EC50 > 1000.0 nM -
CHEMBL3824241 EC50 > 1000.0 nM -
CHEMBL3823722 EC50 > 1000.0 nM -
CHEMBL3822888 EC50 > 1000.0 nM -
CHEMBL4299689 EC50 > 1000.0 nM -
CHEMBL3823994 EC50 > 1000.0 nM -
CHEMBL4299648 EC50 > 1000.0 nM -
CHEMBL4299622 EC50 > 1000.0 nM -
CHEMBL3823847 EC50 > 1000.0 nM -
CHEMBL3823327 EC50 > 1000.0 nM -
CHEMBL3823985 EC50 > 1000.0 nM -
CHEMBL3823144 EC50 > 1000.0 nM -
CHEMBL3822792 EC50 > 1000.0 nM -
CHEMBL3823976 EC50 > 1000.0 nM -
CHEMBL3822459 EC50 > 1000.0 nM -
CHEMBL4299662 EC50 > 1000.0 nM -
CHEMBL3823643 EC50 > 1000.0 nM -
CHEMBL3824278 EC50 > 1000.0 nM -
CHEMBL3822928 EC50 > 1000.0 nM -
CHEMBL4299631 EC50 > 1000.0 nM -
CHEMBL3822636 EC50 > 1000.0 nM -