Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4370032

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

Functional
Agonist activity at human CCK1R 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

Cholecystokinin receptor type A (CHEMBL1901) ↗
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 9.15 10.60
pEC50 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423907 — — 1 10.60
CHEMBL1121 SINCALIDE 4.0 1 10.36
CHEMBL4464703 — — 1 10.22
CHEMBL4453982 — — 1 10.17
CHEMBL4475304 — — 1 9.97
CHEMBL4471525 — — 1 9.97
CHEMBL4467338 — — 1 9.96
CHEMBL4551834 — — 1 9.94
CHEMBL4557012 — — 1 9.94
CHEMBL4443415 — — 1 9.89
CHEMBL4565336 — — 1 9.89
CHEMBL4473468 — — 1 9.87
CHEMBL4572516 — — 1 9.81
CHEMBL4455361 — — 1 9.80
CHEMBL4563364 — — 1 9.79
CHEMBL4459331 — — 1 9.79
CHEMBL4471373 — — 1 9.78
CHEMBL4468861 — — 1 9.78
CHEMBL4471871 — — 1 9.77
CHEMBL4544208 — — 1 9.74
CHEMBL4520976 — — 1 9.72
CHEMBL4542927 — — 1 9.67
CHEMBL4440303 — — 1 9.67
CHEMBL4483457 — — 1 9.61
CHEMBL4440419 — — 1 9.60
CHEMBL4514283 — — 1 9.54
CHEMBL4525615 — — 1 9.53
CHEMBL4534977 — — 1 9.50
CHEMBL4444353 — — 1 9.50
CHEMBL4534236 — — 1 9.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423907 — EC50 = 0.02512 nM 10.60
CHEMBL1121 SINCALIDE EC50 = 0.04365 nM 10.36
CHEMBL4464703 — EC50 = 0.06026 nM 10.22
CHEMBL4453982 — EC50 = 0.06761 nM 10.17
CHEMBL4475304 — EC50 = 0.1072 nM 9.97
CHEMBL4471525 — EC50 = 0.1072 nM 9.97
CHEMBL4467338 — EC50 = 0.1096 nM 9.96
CHEMBL4551834 — EC50 = 0.1148 nM 9.94
CHEMBL4557012 — EC50 = 0.1148 nM 9.94
CHEMBL4443415 — EC50 = 0.1288 nM 9.89
CHEMBL4565336 — EC50 = 0.1288 nM 9.89
CHEMBL4473468 — EC50 = 0.1349 nM 9.87
CHEMBL4572516 — EC50 = 0.1549 nM 9.81
CHEMBL4455361 — EC50 = 0.1585 nM 9.80
CHEMBL4459331 — EC50 = 0.1622 nM 9.79
CHEMBL4563364 — EC50 = 0.1622 nM 9.79
CHEMBL4471373 — EC50 = 0.166 nM 9.78
CHEMBL4468861 — EC50 = 0.166 nM 9.78
CHEMBL4471871 — EC50 = 0.1698 nM 9.77
CHEMBL4544208 — EC50 = 0.182 nM 9.74
CHEMBL4520976 — EC50 = 0.1905 nM 9.72
CHEMBL4542927 — EC50 = 0.2138 nM 9.67
CHEMBL4440303 — EC50 = 0.2138 nM 9.67
CHEMBL4483457 — EC50 = 0.2455 nM 9.61
CHEMBL4440419 — EC50 = 0.2512 nM 9.60
CHEMBL4514283 — EC50 = 0.2884 nM 9.54
CHEMBL4525615 — EC50 = 0.2951 nM 9.53
CHEMBL4534977 — EC50 = 0.3162 nM 9.50
CHEMBL4444353 — EC50 = 0.3162 nM 9.50
CHEMBL4534236 — EC50 = 0.3236 nM 9.49
CHEMBL4441596 — EC50 = 0.3631 nM 9.44
CHEMBL4583158 — EC50 = 0.3631 nM 9.44
CHEMBL4526455 — EC50 = 0.3715 nM 9.43
CHEMBL4536393 — EC50 = 0.389 nM 9.41
CHEMBL4585323 — EC50 = 0.4074 nM 9.39
CHEMBL4550876 — EC50 = 0.4467 nM 9.35
CHEMBL4445529 — EC50 = 0.5012 nM 9.30
CHEMBL4591101 — EC50 = 0.5012 nM 9.30
CHEMBL4568746 — EC50 = 0.5012 nM 9.30
CHEMBL4467402 — EC50 = 0.7244 nM 9.14
CHEMBL4522865 — EC50 = 0.9772 nM 9.01
CHEMBL4516794 — EC50 = 1.122 nM 8.95
CHEMBL4553223 — EC50 = 1.549 nM 8.81
CHEMBL4540877 — EC50 = 1.622 nM 8.79
CHEMBL4520699 — EC50 = 3.311 nM 8.48
CHEMBL4468598 — EC50 = 8.511 nM 8.07
CHEMBL2369816 — EC50 = 9.12 nM 8.04
CHEMBL4547294 — EC50 = 11.75 nM 7.93
CHEMBL4465747 — EC50 = 11.75 nM 7.93
CHEMBL4570130 — EC50 = 117.49 nM 6.93