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Assay Detail

CHEMBL4370033

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Functional
Agonist activity at human CCK2R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL ↗
63
Total Activities
63
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
Sensfuss U, Kruse T, Skyggebjerg RB, Uldam HK, Vestergaard B, Huus K, Vinther TN, Reinau ME, Schéele S, Clausen TR.
J Med Chem (2019) 62 : 1407 -1419
PubMed 30624060 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 56 8.45 9.53
pEC50 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4468861 — — 1 9.53
CHEMBL4570130 — — 1 9.50
CHEMBL4522865 — — 1 9.49
CHEMBL4547294 — — 1 9.48
CHEMBL4516868 — — 1 9.42
CHEMBL4555341 — — 1 9.42
CHEMBL4563364 — — 1 9.39
CHEMBL4459331 — — 1 9.38
CHEMBL4534236 — — 1 9.38
CHEMBL4443415 — — 1 9.36
CHEMBL4561184 — — 1 9.36
CHEMBL4453982 — — 1 9.35
CHEMBL4551834 — — 1 9.34
CHEMBL4451154 — — 1 9.34
CHEMBL1121 SINCALIDE 4.0 1 9.30
CHEMBL4565336 — — 1 9.30
CHEMBL4467338 — — 1 9.20
CHEMBL4445353 — — 1 9.08
CHEMBL4471871 — — 1 8.81
CHEMBL4568746 — — 1 8.73
CHEMBL4591101 — — 1 8.57
CHEMBL4471525 — — 1 8.30
CHEMBL4465747 — — 1 8.24
CHEMBL4445529 — — 1 7.78
CHEMBL4516794 — — 1 7.59
CHEMBL4441596 — — 1 7.05
CHEMBL4514283 — — 1 6.98
CHEMBL4583158 — — 1 6.91
CHEMBL4550876 — — 1 6.88
CHEMBL4585323 — — 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4468861 — EC50 = 0.2951 nM 9.53
CHEMBL4570130 — EC50 = 0.3162 nM 9.50
CHEMBL4522865 — EC50 = 0.3236 nM 9.49
CHEMBL4547294 — EC50 = 0.3311 nM 9.48
CHEMBL4516868 — EC50 = 0.3802 nM 9.42
CHEMBL4555341 — EC50 = 0.3802 nM 9.42
CHEMBL4563364 — EC50 = 0.4074 nM 9.39
CHEMBL4459331 — EC50 = 0.4169 nM 9.38
CHEMBL4534236 — EC50 = 0.4169 nM 9.38
CHEMBL4443415 — EC50 = 0.4365 nM 9.36
CHEMBL4561184 — EC50 = 0.4365 nM 9.36
CHEMBL4453982 — EC50 = 0.4467 nM 9.35
CHEMBL4551834 — EC50 = 0.4571 nM 9.34
CHEMBL4451154 — EC50 = 0.4571 nM 9.34
CHEMBL4565336 — EC50 = 0.5012 nM 9.30
CHEMBL1121 SINCALIDE EC50 = 0.5012 nM 9.30
CHEMBL4467338 — EC50 = 0.631 nM 9.20
CHEMBL4445353 — EC50 = 0.8318 nM 9.08
CHEMBL4471871 — EC50 = 1.549 nM 8.81
CHEMBL4568746 — EC50 = 1.862 nM 8.73
CHEMBL4591101 — EC50 = 2.692 nM 8.57
CHEMBL4471525 — EC50 = 5.012 nM 8.30
CHEMBL4465747 — EC50 = 5.754 nM 8.24
CHEMBL4445529 — EC50 = 16.6 nM 7.78
CHEMBL4516794 — EC50 = 25.7 nM 7.59
CHEMBL4441596 — EC50 = 89.13 nM 7.05
CHEMBL4514283 — EC50 = 104.71 nM 6.98
CHEMBL4583158 — EC50 = 123.03 nM 6.91
CHEMBL4550876 — EC50 = 131.83 nM 6.88
CHEMBL4585323 — EC50 = 151.36 nM 6.82
CHEMBL4525615 — EC50 = 173.78 nM 6.76
CHEMBL2369816 — EC50 = 194.98 nM 6.71
CHEMBL4483457 — EC50 = 316.23 nM 6.50
CHEMBL4471373 — EC50 = 870.96 nM 6.06
CHEMBL4544208 — EC50 > 1000.0 nM -
CHEMBL4545970 — EC50 > 1000.0 nM -
CHEMBL4440419 — EC50 > 1000.0 nM -
CHEMBL4475304 — EC50 > 1000.0 nM -
CHEMBL423907 — EC50 > 1000.0 nM -
CHEMBL4467402 — EC50 > 1000.0 nM -
CHEMBL4590542 — pEC50 - — -
CHEMBL4590499 — pEC50 - — -
CHEMBL4534977 — EC50 > 1000.0 nM -
CHEMBL4468598 — EC50 > 1000.0 nM -
CHEMBL4564249 — pEC50 - — -
CHEMBL4553223 — EC50 > 1000.0 nM -
CHEMBL4454469 — pEC50 - — -
CHEMBL4473611 — pEC50 - — -
CHEMBL4559510 — pEC50 - — -
CHEMBL4518377 — pEC50 - — -