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Assay Detail

CHEMBL666754

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

Binding
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
35
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
Bock MG, DiPardo RM, Evans BE, Rittle KE, Whitter WL, Veber DF, Freidinger RM, Chang RS, Chen TB, Lotti VJ.
J Med Chem (1990) 33 : 450 -455
PubMed 2153212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.54 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 8.10
CHEMBL141629 1 7.75
CHEMBL304546 1 7.54
CHEMBL169703 TIFLUADOM 2.0 1 7.33
CHEMBL343066 1 6.80
CHEMBL68870 1 6.58
CHEMBL141354 1 6.35
CHEMBL337530 1 6.22
CHEMBL140365 1 6.10
CHEMBL342415 1 6.00
CHEMBL141051 1 5.66
CHEMBL139615 1 5.54
CHEMBL141365 1 5.40
CHEMBL342256 1 5.39
CHEMBL140516 1 5.37
CHEMBL140749 1 5.32
CHEMBL336690 1 5.24
CHEMBL344154 1 5.16
CHEMBL140974 2 5.10
CHEMBL343158 1 5.00
CHEMBL140620 1 5.00
CHEMBL141786 1 4.94
CHEMBL139520 1 4.89
CHEMBL341815 1 4.85
CHEMBL423918 1 4.82
CHEMBL334933 1 4.66
CHEMBL140984 1 4.66
CHEMBL336256 1 4.62
CHEMBL140495 1 4.55
CHEMBL343969 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE IC50 = 8.0 nM 8.10
CHEMBL141629 IC50 = 18.0 nM 7.75
CHEMBL304546 IC50 = 29.0 nM 7.54
CHEMBL169703 TIFLUADOM IC50 = 47.0 nM 7.33
CHEMBL343066 IC50 = 160.0 nM 6.80
CHEMBL68870 IC50 = 260.0 nM 6.58
CHEMBL141354 IC50 = 450.0 nM 6.35
CHEMBL337530 IC50 = 600.0 nM 6.22
CHEMBL140365 IC50 = 800.0 nM 6.10
CHEMBL342415 IC50 = 1000.0 nM 6.00
CHEMBL141051 IC50 = 2200.0 nM 5.66
CHEMBL139615 IC50 = 2900.0 nM 5.54
CHEMBL141365 IC50 = 4000.0 nM 5.40
CHEMBL342256 IC50 = 4100.0 nM 5.39
CHEMBL140516 IC50 = 4300.0 nM 5.37
CHEMBL140749 IC50 = 4800.0 nM 5.32
CHEMBL336690 IC50 = 5800.0 nM 5.24
CHEMBL344154 IC50 = 7000.0 nM 5.16
CHEMBL140974 IC50 = 8000.0 nM 5.10
CHEMBL343158 IC50 = 10000.0 nM 5.00
CHEMBL140620 IC50 = 10000.0 nM 5.00
CHEMBL141786 IC50 = 11600.0 nM 4.94
CHEMBL139520 IC50 = 13000.0 nM 4.89
CHEMBL341815 IC50 = 14000.0 nM 4.85
CHEMBL423918 IC50 = 15000.0 nM 4.82
CHEMBL140984 IC50 = 22000.0 nM 4.66
CHEMBL334933 IC50 = 22000.0 nM 4.66
CHEMBL336256 IC50 = 24000.0 nM 4.62
CHEMBL140495 IC50 = 28000.0 nM 4.55
CHEMBL343969 IC50 = 45000.0 nM 4.35
CHEMBL336881 IC50 = 100000.0 nM 4.00
CHEMBL141048 IC50 = 100000.0 nM 4.00
CHEMBL140974 IC50 > 100000.0 nM -
CHEMBL139514 IC50 > 100000.0 nM -
CHEMBL434231 IC50 > 100000.0 nM -