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Assay Detail

CHEMBL658773

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

Binding
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKB receptor in guinea pig cortical tissue
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Amino acid-derived piperidides as novel CCKB ligands with anxiolytic-like properties
Holladay MW, Bennett MJ, Bai H, Ralston JW, Kerwin JF, Stashko M, Miller TR, O'Neill AB, Nadzan AM, Brioni J, Lin CW
Bioorg Med Chem Lett (1995) 5 : 3057 -3062
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.27 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320154 1 7.47
CHEMBL420658 1 7.28
CHEMBL418987 1 7.00
CHEMBL103312 1 6.92
CHEMBL322913 1 6.80
CHEMBL105132 1 6.77
CHEMBL104958 1 6.75
CHEMBL102879 1 6.64
CHEMBL102862 1 6.52
CHEMBL103457 1 6.41
CHEMBL105404 1 6.39
CHEMBL321800 1 6.36
CHEMBL321107 1 6.09
CHEMBL103276 1 6.05
CHEMBL320886 1 6.04
CHEMBL102461 1 5.96
CHEMBL105303 1 5.82
CHEMBL102526 1 5.70
CHEMBL101752 1 5.70
CHEMBL105618 1 5.47
CHEMBL105527 1 5.41
CHEMBL101803 1 5.32
CHEMBL320901 1 5.24
CHEMBL105153 1 -
CHEMBL102703 1 -
CHEMBL319466 1 -
CHEMBL431812 1 -
CHEMBL319196 1 -
CHEMBL101854 1 -
CHEMBL420098 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320154 IC50 = 34.0 nM 7.47
CHEMBL420658 IC50 = 53.0 nM 7.28
CHEMBL418987 IC50 = 100.0 nM 7.00
CHEMBL103312 IC50 = 120.0 nM 6.92
CHEMBL322913 IC50 = 160.0 nM 6.80
CHEMBL105132 IC50 = 170.0 nM 6.77
CHEMBL104958 IC50 = 180.0 nM 6.75
CHEMBL102879 IC50 = 230.0 nM 6.64
CHEMBL102862 IC50 = 300.0 nM 6.52
CHEMBL103457 IC50 = 390.0 nM 6.41
CHEMBL105404 IC50 = 410.0 nM 6.39
CHEMBL321800 IC50 = 440.0 nM 6.36
CHEMBL321107 IC50 = 810.0 nM 6.09
CHEMBL103276 IC50 = 900.0 nM 6.05
CHEMBL320886 IC50 = 912.0 nM 6.04
CHEMBL102461 IC50 = 1100.0 nM 5.96
CHEMBL105303 IC50 = 1500.0 nM 5.82
CHEMBL102526 IC50 = 2000.0 nM 5.70
CHEMBL101752 IC50 = 2000.0 nM 5.70
CHEMBL105618 IC50 = 3400.0 nM 5.47
CHEMBL105527 IC50 = 3900.0 nM 5.41
CHEMBL101803 IC50 = 4800.0 nM 5.32
CHEMBL320901 IC50 = 5700.0 nM 5.24
CHEMBL105153 IC50 > 10000.0 nM -
CHEMBL102703 IC50 > 10000.0 nM -
CHEMBL319466 IC50 > 10000.0 nM -
CHEMBL431812 IC50 > 5900.0 nM -
CHEMBL319196 IC50 > 10000.0 nM -
CHEMBL101854 IC50 > 10000.0 nM -
CHEMBL420098 IC50 > 6900.0 nM -
CHEMBL323127 IC50 > 6000.0 nM -
CHEMBL2111654 IC50 > 10000.0 nM -
CHEMBL321072 IC50 > 10000.0 nM -