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Assay Detail

CHEMBL657373

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

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cholecystokinin receptor type A (CHEMBL2871) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 6.62 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330773 — — 1 8.13
CHEMBL332403 — — 1 7.93
CHEMBL332568 — — 1 7.71
CHEMBL331975 — — 1 7.65
CHEMBL121331 — — 1 7.65
CHEMBL332902 — — 1 7.64
CHEMBL121021 — — 1 7.44
CHEMBL331262 — — 1 7.35
CHEMBL338278 — — 1 7.33
CHEMBL121267 — — 1 7.32
CHEMBL421271 — — 1 7.32
CHEMBL120168 — — 1 7.31
CHEMBL333930 — — 1 7.20
CHEMBL331971 — — 1 7.15
CHEMBL333979 — — 3 7.14
CHEMBL331651 — — 1 7.11
CHEMBL334020 — — 1 7.08
CHEMBL118622 — — 1 7.01
CHEMBL331688 — — 1 7.01
CHEMBL120296 — — 1 7.00
CHEMBL420728 — — 1 6.95
CHEMBL121703 — — 1 6.95
CHEMBL332595 — — 1 6.94
CHEMBL331872 — — 1 6.92
CHEMBL339879 — — 1 6.91
CHEMBL120015 — — 1 6.85
CHEMBL103750 — — 3 6.74
CHEMBL121028 — — 2 6.72
CHEMBL332646 — — 1 6.71
CHEMBL332601 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330773 — Ki = 7.413 nM 8.13
CHEMBL332403 — Ki = 11.75 nM 7.93
CHEMBL332568 — Ki = 19.5 nM 7.71
CHEMBL331975 — Ki = 22.39 nM 7.65
CHEMBL121331 — Ki = 22.39 nM 7.65
CHEMBL332902 — Ki = 22.91 nM 7.64
CHEMBL121021 — Ki = 36.31 nM 7.44
CHEMBL331262 — Ki = 44.67 nM 7.35
CHEMBL338278 — Ki = 46.77 nM 7.33
CHEMBL421271 — Ki = 47.86 nM 7.32
CHEMBL121267 — Ki = 47.86 nM 7.32
CHEMBL120168 — Ki = 48.98 nM 7.31
CHEMBL333930 — Ki = 63.1 nM 7.20
CHEMBL331971 — Ki = 70.79 nM 7.15
CHEMBL333979 — Ki = 72.44 nM 7.14
CHEMBL331651 — Ki = 77.62 nM 7.11
CHEMBL334020 — Ki = 83.18 nM 7.08
CHEMBL331688 — Ki = 97.72 nM 7.01
CHEMBL118622 — Ki = 97.72 nM 7.01
CHEMBL120296 — Ki = 100.0 nM 7.00
CHEMBL420728 — Ki = 112.2 nM 6.95
CHEMBL121703 — Ki = 112.2 nM 6.95
CHEMBL332595 — Ki = 114.82 nM 6.94
CHEMBL331872 — Ki = 120.23 nM 6.92
CHEMBL339879 — Ki = 123.03 nM 6.91
CHEMBL333979 — Ki = 125.89 nM 6.90
CHEMBL120015 — Ki = 141.25 nM 6.85
CHEMBL103750 — Ki = 181.97 nM 6.74
CHEMBL121028 — Ki = 190.55 nM 6.72
CHEMBL332646 — Ki = 194.98 nM 6.71
CHEMBL333979 — Ki = 199.53 nM 6.70
CHEMBL332601 — Ki = 218.78 nM 6.66
CHEMBL120793 — Ki = 218.78 nM 6.66
CHEMBL120031 — Ki = 251.19 nM 6.60
CHEMBL278018 — Ki = 251.19 nM 6.60
CHEMBL121624 — Ki = 251.19 nM 6.60
CHEMBL331929 — Ki = 269.15 nM 6.57
CHEMBL332128 — Ki = 295.12 nM 6.53
CHEMBL331405 — Ki = 302.0 nM 6.52
CHEMBL103750 — Ki = 323.59 nM 6.49
CHEMBL402702 — Ki = 338.84 nM 6.47
CHEMBL120021 — Ki = 446.68 nM 6.35
CHEMBL330977 — Ki = 478.63 nM 6.32
CHEMBL330854 — Ki = 549.54 nM 6.26
CHEMBL331763 — Ki = 630.96 nM 6.20
CHEMBL120363 — Ki = 630.96 nM 6.20
CHEMBL340107 — Ki = 660.69 nM 6.18
CHEMBL330977 — Ki = 707.95 nM 6.15
CHEMBL119608 — Ki = 812.83 nM 6.09
CHEMBL333517 — Ki = 1122.02 nM 5.95