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Assay Detail

CHEMBL662464

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

Binding
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type B receptor from rat cerebral cortex membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL3508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
Bartolomé-Nebreda JM, Gómez-Monterrey I, García-López MT, González-Muñiz R, Martín-Martínez M, Ballaz S, Cenarruzabeitia E, LaTorre M, Del Río J, Herranz R.
J Med Chem (1999) 42 : 4659 -4668
PubMed 10579828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.09 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 8.25
CHEMBL9506 DEVAZEPIDE 2.0 1 6.16
CHEMBL2112823 1 5.46
CHEMBL140320 1 5.36
CHEMBL332261 1 5.21
CHEMBL143270 1 -
CHEMBL1794878 1 -
CHEMBL2112828 1 -
CHEMBL2111993 1 -
CHEMBL342912 1 -
CHEMBL337362 1 -
CHEMBL139779 1 -
CHEMBL2112273 1 -
CHEMBL113718 IQM-95333 1 -
CHEMBL2112824 1 -
CHEMBL140262 1 -
CHEMBL140098 1 -
CHEMBL2112829 1 -
CHEMBL143672 1 -
CHEMBL3350871 1 -
CHEMBL343560 1 -
CHEMBL2112825 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 5.6 nM 8.25
CHEMBL9506 DEVAZEPIDE IC50 = 696.0 nM 6.16
CHEMBL2112823 IC50 = 3430.0 nM 5.46
CHEMBL140320 IC50 = 4390.0 nM 5.36
CHEMBL332261 IC50 = 6153.0 nM 5.21
CHEMBL143270 IC50 > 10000.0 nM -
CHEMBL1794878 IC50 > 10000.0 nM -
CHEMBL2112828 IC50 > 10000.0 nM -
CHEMBL2111993 IC50 > 10000.0 nM -
CHEMBL342912 IC50 > 10000.0 nM -
CHEMBL337362 IC50 > 10000.0 nM -
CHEMBL139779 IC50 > 10000.0 nM -
CHEMBL2112273 IC50 > 10000.0 nM -
CHEMBL113718 IQM-95333 IC50 > 10000.0 nM -
CHEMBL2112824 IC50 > 10000.0 nM -
CHEMBL140262 IC50 > 10000.0 nM -
CHEMBL140098 IC50 > 10000.0 nM -
CHEMBL2112829 IC50 > 10000.0 nM -
CHEMBL143672 IC50 > 10000.0 nM -
CHEMBL3350871 IC50 > 10000.0 nM -
CHEMBL343560 IC50 > 10000.0 nM -
CHEMBL2112825 IC50 > 10000.0 nM -