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Assay Detail

CHEMBL662468

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

Binding
Inhibition of [3H]pCCK-8 specific binding cholecystokinin type B receptor in rat cerebral cortex membranes
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
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: structure-activity relationship studies on the substituent at N2-position.
Bartolomé-Nebreda JM, Patiño-Molina R, Martín-Martínez M, Gómez-Monterrey I, García-López MT, González-Muñiz R, Cenarruzabeitia E, Latorre M, Del Río J, Herranz R.
J Med Chem (2001) 44 : 2219 -2228
PubMed 11405658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.96 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216166 1 8.25
CHEMBL2112234 1 5.88
CHEMBL2115130 1 5.63
CHEMBL2112239 1 5.63
CHEMBL116127 1 5.21
CHEMBL2112233 1 5.14
CHEMBL71229 1 -
CHEMBL2114083 1 -
CHEMBL2114079 1 -
CHEMBL2111545 1 -
CHEMBL2114082 1 -
CHEMBL2112235 1 -
CHEMBL265322 1 -
CHEMBL113718 IQM-95333 1 -
CHEMBL366344 1 -
CHEMBL189634 1 -
CHEMBL3350282 1 -
CHEMBL2115131 1 -
CHEMBL2112238 1 -
CHEMBL2114081 1 -
CHEMBL2111548 1 -
CHEMBL2112231 1 -
CHEMBL2115132 1 -
CHEMBL2111551 1 -
CHEMBL2112230 1 -
CHEMBL70575 1 -
CHEMBL2115133 1 -
CHEMBL2111549 1 -
CHEMBL71996 1 -
CHEMBL2111552 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216166 IC50 = 5.6 nM 8.25
CHEMBL2112234 IC50 = 1320.0 nM 5.88
CHEMBL2115130 IC50 = 2320.0 nM 5.63
CHEMBL2112239 IC50 = 2320.0 nM 5.63
CHEMBL116127 IC50 = 6153.0 nM 5.21
CHEMBL2112233 IC50 = 7159.0 nM 5.14
CHEMBL265322 IC50 > 10000.0 nM -
CHEMBL2111550 IC50 > 10000.0 nM -
CHEMBL113718 IQM-95333 IC50 > 10000.0 nM -
CHEMBL366344 IC50 > 10000.0 nM -
CHEMBL189634 IC50 > 10000.0 nM -
CHEMBL3350282 IC50 > 10000.0 nM -
CHEMBL2115131 IC50 > 10000.0 nM -
CHEMBL2114083 IC50 > 10000.0 nM -
CHEMBL2111547 IC50 > 10000.0 nM -
CHEMBL3350281 IC50 > 10000.0 nM -
CHEMBL308115 IC50 > 10000.0 nM -
CHEMBL2112236 IC50 > 10000.0 nM -
CHEMBL2112237 IC50 > 10000.0 nM -
CHEMBL2111546 IC50 > 10000.0 nM -
CHEMBL2112232 IC50 > 10000.0 nM -
CHEMBL2114084 IC50 > 10000.0 nM -
CHEMBL2112231 IC50 > 10000.0 nM -
CHEMBL2111552 IC50 > 10000.0 nM -
CHEMBL71996 IC50 > 10000.0 nM -
CHEMBL2111549 IC50 > 10000.0 nM -
CHEMBL2115133 IC50 > 10000.0 nM -
CHEMBL70575 IC50 > 10000.0 nM -
CHEMBL2112230 IC50 > 10000.0 nM -
CHEMBL2111551 IC50 > 10000.0 nM -
CHEMBL2115132 IC50 > 10000.0 nM -
CHEMBL2112235 IC50 > 10000.0 nM -
CHEMBL2111548 IC50 > 10000.0 nM -
CHEMBL2114081 IC50 > 10000.0 nM -
CHEMBL2112238 IC50 > 10000.0 nM -
CHEMBL71229 IC50 > 10000.0 nM -
CHEMBL2114079 IC50 > 10000.0 nM -
CHEMBL2111545 IC50 > 10000.0 nM -
CHEMBL2114082 IC50 > 10000.0 nM -