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Assay Detail

CHEMBL799243

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

Functional
Inhibition of amylase release stimulated by CCK-8 (0.1 nM) in dispersed pancreatic acini
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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 17 7.85 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113718 IQM-95333 1 9.19
CHEMBL366344 1 9.14
CHEMBL2114081 1 8.72
CHEMBL2111545 1 8.52
CHEMBL189634 1 8.46
CHEMBL2115133 1 8.05
CHEMBL2111550 1 8.00
CHEMBL2112237 1 7.90
CHEMBL2111549 1 7.78
CHEMBL71996 1 7.42
CHEMBL2114079 1 7.40
CHEMBL2111548 1 7.30
CHEMBL2111547 1 7.19
CHEMBL116127 1 7.11
CHEMBL2114084 1 6.95
CHEMBL2112233 1 6.54
CHEMBL2111552 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113718 IQM-95333 IC50 = 0.64 nM 9.19
CHEMBL366344 IC50 = 0.73 nM 9.14
CHEMBL2114081 IC50 = 1.89 nM 8.72
CHEMBL2111545 IC50 = 3.0 nM 8.52
CHEMBL189634 IC50 = 3.5 nM 8.46
CHEMBL2115133 IC50 = 9.0 nM 8.05
CHEMBL2111550 IC50 = 10.0 nM 8.00
CHEMBL2112237 IC50 = 12.63 nM 7.90
CHEMBL2111549 IC50 = 16.6 nM 7.78
CHEMBL71996 IC50 = 38.1 nM 7.42
CHEMBL2114079 IC50 = 39.8 nM 7.40
CHEMBL2111548 IC50 = 49.5 nM 7.30
CHEMBL2111547 IC50 = 64.0 nM 7.19
CHEMBL116127 IC50 = 77.0 nM 7.11
CHEMBL2114084 IC50 = 112.0 nM 6.95
CHEMBL2112233 IC50 = 287.0 nM 6.54
CHEMBL2111552 IC50 > 1000.0 nM -