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Assay Detail

CHEMBL662467

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

Binding
Inhibition of the specific binding of [125I](BH)-CCK-8 to Cholecystokinin type B receptor in rat brain cortex
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
Makovec F, Peris W, Revel L, Giovanetti R, Mennuni L, Rovati LC.
J Med Chem (1992) 35 : 28 -38
PubMed 1732532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 5.54 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 9.00
CHEMBL1328 PENTAGASTRIN 4.0 1 8.17
CHEMBL125925 1 6.70
CHEMBL339453 1 6.52
CHEMBL124396 1 6.52
CHEMBL339041 1 6.40
CHEMBL340630 1 6.40
CHEMBL125874 1 6.40
CHEMBL340463 1 6.30
CHEMBL124832 1 6.30
CHEMBL340413 1 6.22
CHEMBL339134 1 6.16
CHEMBL421474 1 6.10
CHEMBL123684 1 6.10
CHEMBL334171 1 6.10
CHEMBL331413 1 6.05
CHEMBL124764 1 6.00
CHEMBL338134 1 5.92
CHEMBL421438 1 5.92
CHEMBL124509 1 5.80
CHEMBL338929 1 5.72
CHEMBL341143 1 5.72
CHEMBL124732 1 5.64
CHEMBL2111826 1 5.64
CHEMBL124780 1 5.64
CHEMBL122922 1 5.64
CHEMBL124155 1 5.57
CHEMBL2111825 1 5.55
CHEMBL124378 1 5.54
CHEMBL2111827 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 1.0 nM 9.00
CHEMBL1328 PENTAGASTRIN IC50 = 6.8 nM 8.17
CHEMBL125925 IC50 = 200.0 nM 6.70
CHEMBL339453 IC50 = 300.0 nM 6.52
CHEMBL124396 IC50 = 300.0 nM 6.52
CHEMBL339041 IC50 = 400.0 nM 6.40
CHEMBL340630 IC50 = 400.0 nM 6.40
CHEMBL125874 IC50 = 400.0 nM 6.40
CHEMBL340463 IC50 = 500.0 nM 6.30
CHEMBL124832 IC50 = 500.0 nM 6.30
CHEMBL340413 IC50 = 600.0 nM 6.22
CHEMBL339134 IC50 = 700.0 nM 6.16
CHEMBL421474 IC50 = 800.0 nM 6.10
CHEMBL334171 IC50 = 800.0 nM 6.10
CHEMBL123684 IC50 = 800.0 nM 6.10
CHEMBL331413 IC50 = 900.0 nM 6.05
CHEMBL124764 IC50 = 1000.0 nM 6.00
CHEMBL338134 IC50 = 1200.0 nM 5.92
CHEMBL421438 IC50 = 1200.0 nM 5.92
CHEMBL124509 IC50 = 1600.0 nM 5.80
CHEMBL338929 IC50 = 1900.0 nM 5.72
CHEMBL341143 IC50 = 1900.0 nM 5.72
CHEMBL122922 IC50 = 2300.0 nM 5.64
CHEMBL124780 IC50 = 2300.0 nM 5.64
CHEMBL124732 IC50 = 2300.0 nM 5.64
CHEMBL2111826 IC50 = 2300.0 nM 5.64
CHEMBL124155 IC50 = 2700.0 nM 5.57
CHEMBL2111825 IC50 = 2800.0 nM 5.55
CHEMBL124378 IC50 = 2900.0 nM 5.54
CHEMBL2111827 IC50 = 3000.0 nM 5.52
CHEMBL340263 IC50 = 3000.0 nM 5.52
CHEMBL24938 LORGLUMIDE IC50 = 3000.0 nM 5.52
CHEMBL125551 IC50 = 3100.0 nM 5.51
CHEMBL125703 IC50 = 3200.0 nM 5.50
CHEMBL339115 IC50 = 3300.0 nM 5.48
CHEMBL123852 IC50 = 3600.0 nM 5.44
CHEMBL123720 IC50 = 3800.0 nM 5.42
CHEMBL2111828 IC50 = 5800.0 nM 5.24
CHEMBL124712 IC50 = 5800.0 nM 5.24
CHEMBL124805 IC50 = 6000.0 nM 5.22
CHEMBL124261 IC50 = 6200.0 nM 5.21
CHEMBL124459 IC50 = 7000.0 nM 5.16
CHEMBL434250 IC50 = 7800.0 nM 5.11
CHEMBL123785 IC50 = 8000.0 nM 5.10
CHEMBL123089 IC50 = 8100.0 nM 5.09
CHEMBL124822 IC50 = 10100.0 nM 5.00
CHEMBL124917 IC50 = 10200.0 nM 4.99
CHEMBL435587 IC50 = 10500.0 nM 4.98
CHEMBL341505 IC50 = 16100.0 nM 4.79
CHEMBL339707 IC50 = 16300.0 nM 4.79