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Assay Detail

CHEMBL663095

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Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type B receptor of guinea pig cerebral cortex membranes
ChEMBL ↗
63
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
Ursini A, Capelli AM, Carr RA, Cassarà P, Corsi M, Curcuruto O, Curotto G, Dal Cin M, Davalli S, Donati D, Feriani A, Finch H, Finizia G, Gaviraghi G, Marien M, Pentassuglia G, Polinelli S, Ratti E, Reggiani AM, Tarzia G, Tedesco G, Tranquillini ME, Trist DG, Van Amsterdam FT.
J Med Chem (2000) 43 : 3596 -3613
PubMed 11020274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 63 8.79 9.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415240 — — 1 9.75
CHEMBL333979 — — 3 9.68
CHEMBL331872 — — 1 9.65
CHEMBL332902 — — 1 9.54
CHEMBL331468 — — 1 9.53
CHEMBL331975 — — 1 9.52
CHEMBL121021 — — 1 9.48
CHEMBL330773 — — 1 9.31
CHEMBL402702 — — 1 9.25
CHEMBL331244 — — 1 9.24
CHEMBL332568 — — 1 9.22
CHEMBL118622 — — 1 9.19
CHEMBL118954 — — 1 9.18
CHEMBL420728 — — 1 9.17
CHEMBL421271 — — 1 9.17
CHEMBL331763 — — 2 9.17
CHEMBL332403 — — 1 9.14
CHEMBL120296 — — 1 9.14
CHEMBL121331 — — 1 9.12
CHEMBL121028 — — 2 9.08
CHEMBL330977 — — 3 9.03
CHEMBL333517 — — 1 9.02
CHEMBL331971 — — 1 9.02
CHEMBL120363 — — 1 9.01
CHEMBL331262 — — 1 8.99
CHEMBL339879 — — 1 8.95
CHEMBL120021 — — 1 8.95
CHEMBL333930 — — 1 8.90
CHEMBL331119 — — 1 8.88
CHEMBL118189 — — 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415240 — Ki = 0.1778 nM 9.75
CHEMBL333979 — Ki = 0.2089 nM 9.68
CHEMBL331872 — Ki = 0.2239 nM 9.65
CHEMBL333979 — Ki = 0.2512 nM 9.60
CHEMBL332902 — Ki = 0.2884 nM 9.54
CHEMBL331468 — Ki = 0.2951 nM 9.53
CHEMBL331975 — Ki = 0.302 nM 9.52
CHEMBL121021 — Ki = 0.3311 nM 9.48
CHEMBL330773 — Ki = 0.4898 nM 9.31
CHEMBL402702 — Ki = 0.5623 nM 9.25
CHEMBL331244 — Ki = 0.5754 nM 9.24
CHEMBL332568 — Ki = 0.6026 nM 9.22
CHEMBL118622 — Ki = 0.6457 nM 9.19
CHEMBL118954 — Ki = 0.6607 nM 9.18
CHEMBL420728 — Ki = 0.6761 nM 9.17
CHEMBL421271 — Ki = 0.6761 nM 9.17
CHEMBL331763 — Ki = 0.6761 nM 9.17
CHEMBL332403 — Ki = 0.7244 nM 9.14
CHEMBL120296 — Ki = 0.7244 nM 9.14
CHEMBL121331 — Ki = 0.7586 nM 9.12
CHEMBL121028 — Ki = 0.8318 nM 9.08
CHEMBL330977 — Ki = 0.9333 nM 9.03
CHEMBL333517 — Ki = 0.955 nM 9.02
CHEMBL331971 — Ki = 0.955 nM 9.02
CHEMBL120363 — Ki = 0.9772 nM 9.01
CHEMBL331262 — Ki = 1.023 nM 8.99
CHEMBL120021 — Ki = 1.122 nM 8.95
CHEMBL339879 — Ki = 1.122 nM 8.95
CHEMBL333930 — Ki = 1.259 nM 8.90
CHEMBL331763 — Ki = 1.259 nM 8.90
CHEMBL331119 — Ki = 1.318 nM 8.88
CHEMBL118189 — Ki = 1.413 nM 8.85
CHEMBL338278 — Ki = 1.514 nM 8.82
CHEMBL278018 — Ki = 1.549 nM 8.81
CHEMBL103750 — Ki = 1.549 nM 8.81
CHEMBL120031 — Ki = 1.549 nM 8.81
CHEMBL121267 — Ki = 1.738 nM 8.76
CHEMBL333979 — Ki = 1.862 nM 8.73
CHEMBL331405 — Ki = 1.905 nM 8.72
CHEMBL334020 — Ki = 1.95 nM 8.71
CHEMBL331688 — Ki = 2.089 nM 8.68
CHEMBL332595 — Ki = 2.089 nM 8.68
CHEMBL330977 — Ki = 2.291 nM 8.64
CHEMBL120015 — Ki = 2.344 nM 8.63
CHEMBL120168 — Ki = 2.455 nM 8.61
CHEMBL121703 — Ki = 2.884 nM 8.54
CHEMBL119608 — Ki = 2.951 nM 8.53
CHEMBL332850 — Ki = 3.02 nM 8.52
CHEMBL331651 — Ki = 3.548 nM 8.45
CHEMBL121028 — Ki = 3.802 nM 8.42