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Assay Detail

CHEMBL3267240

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

Functional
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucose-dependent insulinotropic receptor (CHEMBL5652)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R.
Bioorg Med Chem Lett (2014) 24 : 2383 -2387
PubMed 24751443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 6.92 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3260536 1 9.00
CHEMBL3260535 1 8.40
CHEMBL3260533 1 8.00
CHEMBL3260532 1 7.96
CHEMBL3260512 1 7.80
CHEMBL3260518 1 7.77
CHEMBL3260517 1 7.70
CHEMBL3260540 1 7.70
CHEMBL3260522 1 7.40
CHEMBL3260527 1 7.40
CHEMBL3260542 1 7.28
CHEMBL3260531 1 7.24
CHEMBL3260541 1 7.21
CHEMBL3260525 1 7.20
CHEMBL3260526 1 7.14
CHEMBL3260537 1 7.07
CHEMBL3260523 1 6.96
CHEMBL3260528 1 6.89
CHEMBL3260521 1 6.85
CHEMBL3260538 1 6.79
CHEMBL3260524 1 6.77
CHEMBL3260529 1 6.75
CHEMBL3260515 1 6.72
CHEMBL3260520 1 6.72
CHEMBL3260506 1 6.70
CHEMBL3260539 1 6.61
CHEMBL3260513 1 6.54
CHEMBL3260511 1 6.47
CHEMBL3260508 1 6.25
CHEMBL3260509 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3260536 EC50 = 1.0 nM 9.00
CHEMBL3260535 EC50 = 4.0 nM 8.40
CHEMBL3260533 EC50 = 10.0 nM 8.00
CHEMBL3260532 EC50 = 11.0 nM 7.96
CHEMBL3260512 EC50 = 16.0 nM 7.80
CHEMBL3260518 EC50 = 17.0 nM 7.77
CHEMBL3260517 EC50 = 20.0 nM 7.70
CHEMBL3260540 EC50 = 20.0 nM 7.70
CHEMBL3260522 EC50 = 40.0 nM 7.40
CHEMBL3260527 EC50 = 40.0 nM 7.40
CHEMBL3260542 EC50 = 53.0 nM 7.28
CHEMBL3260531 EC50 = 58.0 nM 7.24
CHEMBL3260541 EC50 = 62.0 nM 7.21
CHEMBL3260525 EC50 = 63.0 nM 7.20
CHEMBL3260526 EC50 = 73.0 nM 7.14
CHEMBL3260537 EC50 = 86.0 nM 7.07
CHEMBL3260523 EC50 = 110.0 nM 6.96
CHEMBL3260528 EC50 = 130.0 nM 6.89
CHEMBL3260521 EC50 = 140.0 nM 6.85
CHEMBL3260538 EC50 = 164.0 nM 6.79
CHEMBL3260524 EC50 = 170.0 nM 6.77
CHEMBL3260529 EC50 = 180.0 nM 6.75
CHEMBL3260520 EC50 = 190.0 nM 6.72
CHEMBL3260515 EC50 = 190.0 nM 6.72
CHEMBL3260506 EC50 = 200.0 nM 6.70
CHEMBL3260539 EC50 = 243.0 nM 6.61
CHEMBL3260513 EC50 = 290.0 nM 6.54
CHEMBL3260511 EC50 = 340.0 nM 6.47
CHEMBL3260508 EC50 = 560.0 nM 6.25
CHEMBL3260509 EC50 = 880.0 nM 6.06
CHEMBL3260543 EC50 = 1100.0 nM 5.96
CHEMBL3260514 EC50 = 1200.0 nM 5.92
CHEMBL3260507 EC50 = 1300.0 nM 5.89
CHEMBL461384 EC50 = 3000.0 nM 5.52
CHEMBL3260505 MBX-2982 EC50 = 5000.0 nM 5.30
CHEMBL3260504 EC50 = 9000.0 nM 5.05
CHEMBL1081913 EC50 = 630000.0 nM -
CHEMBL3260510 EC50 > 10000.0 nM -
CHEMBL3260516 EC50 > 10000.0 nM -
CHEMBL3260519 EC50 > 10000.0 nM -
CHEMBL3260530 EC50 > 10000.0 nM -
CHEMBL3260534 EC50 > 300.0 nM -