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Assay Detail

CHEMBL2161791

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

Binding
Inhibition of [125I]GLP1 (7-36) amide binding to rat GLP1R expressed in HEK293 cells
ChEMBL ↗
55
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucagon-like peptide 1 receptor (CHEMBL5862) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cyclobutane derivatives as novel nonpeptidic small molecule agonists of glucagon-like peptide-1 receptor.
Liu Q, Li N, Yuan Y, Lu H, Wu X, Zhou C, He M, Su H, Zhang M, Wang J, Wang B, Wang Y, Ma D, Ye Y, Weiss HC, Gesing ER, Liao J, Wang MW.
J Med Chem (2012) 55 : 250 -267
PubMed 22103243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 55 5.59 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2158418 — — 1 6.52
CHEMBL2158488 — — 1 6.52
CHEMBL2158489 — — 1 6.30
CHEMBL2158411 — — 2 6.22
CHEMBL2158498 — — 1 6.05
CHEMBL2158421 — — 1 6.00
CHEMBL2158410 — — 1 6.00
CHEMBL2158419 — — 1 5.92
CHEMBL2158420 — — 1 5.92
CHEMBL2158412 — — 1 5.89
CHEMBL2158494 — — 1 5.85
CHEMBL2158491 — — 1 5.72
CHEMBL2158422 — — 1 5.64
CHEMBL2158407 — — 1 5.57
CHEMBL2158495 — — 1 5.52
CHEMBL2158404 — — 1 5.51
CHEMBL2158493 — — 1 5.50
CHEMBL2158487 — — 1 5.47
CHEMBL2158311 — — 1 5.44
CHEMBL2158414 — — 1 5.44
CHEMBL2158413 — — 1 5.37
CHEMBL2158497 — — 1 5.37
CHEMBL2158423 — — 1 5.31
CHEMBL2158408 — — 1 5.12
CHEMBL2158409 — — 1 5.12
CHEMBL2158490 — — 1 5.10
CHEMBL2158500 — — 1 5.09
CHEMBL2158492 — — 1 5.07
CHEMBL2158316 — — 1 5.02
CHEMBL2158499 — — 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2158418 — IC50 = 300.0 nM 6.52
CHEMBL2158488 — IC50 = 300.0 nM 6.52
CHEMBL2158489 — IC50 = 500.0 nM 6.30
CHEMBL2158411 — IC50 = 600.0 nM 6.22
CHEMBL2158498 — IC50 = 900.0 nM 6.05
CHEMBL2158410 — IC50 = 1000.0 nM 6.00
CHEMBL2158421 — IC50 = 1000.0 nM 6.00
CHEMBL2158419 — IC50 = 1200.0 nM 5.92
CHEMBL2158420 — IC50 = 1200.0 nM 5.92
CHEMBL2158412 — IC50 = 1300.0 nM 5.89
CHEMBL2158494 — IC50 = 1400.0 nM 5.85
CHEMBL2158411 — IC50 = 1600.0 nM 5.80
CHEMBL2158491 — IC50 = 1900.0 nM 5.72
CHEMBL2158422 — IC50 = 2310.0 nM 5.64
CHEMBL2158407 — IC50 = 2700.0 nM 5.57
CHEMBL2158495 — IC50 = 3000.0 nM 5.52
CHEMBL2158404 — IC50 = 3100.0 nM 5.51
CHEMBL2158493 — IC50 = 3200.0 nM 5.50
CHEMBL2158487 — IC50 = 3400.0 nM 5.47
CHEMBL2158414 — IC50 = 3600.0 nM 5.44
CHEMBL2158311 — IC50 = 3600.0 nM 5.44
CHEMBL2158497 — IC50 = 4300.0 nM 5.37
CHEMBL2158413 — IC50 = 4300.0 nM 5.37
CHEMBL2158423 — IC50 = 4900.0 nM 5.31
CHEMBL2158409 — IC50 = 7500.0 nM 5.12
CHEMBL2158408 — IC50 = 7500.0 nM 5.12
CHEMBL2158490 — IC50 = 8000.0 nM 5.10
CHEMBL2158500 — IC50 = 8100.0 nM 5.09
CHEMBL2158492 — IC50 = 8500.0 nM 5.07
CHEMBL2158316 — IC50 = 9600.0 nM 5.02
CHEMBL2158499 — IC50 = 16200.0 nM 4.79
CHEMBL2158313 — IC50 = 17500.0 nM 4.76
CHEMBL2158396 — IC50 - — -
CHEMBL2158397 — IC50 - — -
CHEMBL2158398 — IC50 - — -
CHEMBL2158399 — IC50 > 20000.0 nM -
CHEMBL2158400 — IC50 > 20000.0 nM -
CHEMBL2158401 — IC50 - — -
CHEMBL2158402 — IC50 - — -
CHEMBL2158403 — IC50 - — -
CHEMBL2158405 — IC50 - — -
CHEMBL2158417 — IC50 > 20000.0 nM -
CHEMBL2158416 — IC50 > 20000.0 nM -
CHEMBL2158415 — IC50 > 20000.0 nM -
CHEMBL2158406 — IC50 - — -
CHEMBL2158312 — IC50 - — -
CHEMBL2158314 — IC50 - — -
CHEMBL2158315 — IC50 > 20000.0 nM -
CHEMBL2158496 — IC50 - — -
CHEMBL2158317 — IC50 - — -