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Assay Detail

CHEMBL661838

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

Binding
Binding affinity towards Cholecystokinin type B receptor (CCK-B) receptor in mouse cerebral cortex using [125I]bolton Hunter CCK-8 as radioligand
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL2854)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.
Padia JK, Field M, Hinton J, Meecham K, Pablo J, Pinnock R, Roth BD, Singh L, Suman-Chauhan N, Trivedi BK, Webdale L.
J Med Chem (1998) 41 : 1042 -1049
PubMed 9544204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 7.31 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9203 1 9.00
CHEMBL9405 1 8.92
CHEMBL9188 1 8.82
CHEMBL8890 1 8.72
CHEMBL266557 1 8.62
CHEMBL9406 1 8.30
CHEMBL9267 1 8.30
CHEMBL275307 1 8.24
CHEMBL276627 1 8.23
CHEMBL8954 1 8.10
CHEMBL9449 1 8.10
CHEMBL9534 1 8.10
CHEMBL9387 L-365260 1 8.07
CHEMBL9026 1 8.03
CHEMBL9319 1 8.00
CHEMBL266120 1 7.96
CHEMBL8997 1 7.85
CHEMBL9083 1 7.85
CHEMBL9524 1 7.85
CHEMBL9422 1 7.85
CHEMBL9291 1 7.82
CHEMBL9354 1 7.82
CHEMBL9459 1 7.80
CHEMBL8922 1 7.66
CHEMBL9195 1 7.64
CHEMBL9311 1 7.60
CHEMBL9501 1 7.58
CHEMBL267023 1 7.54
CHEMBL269123 1 7.48
CHEMBL415965 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9203 IC50 = 1.0 nM 9.00
CHEMBL9405 IC50 = 1.2 nM 8.92
CHEMBL9188 IC50 = 1.5 nM 8.82
CHEMBL8890 IC50 = 1.9 nM 8.72
CHEMBL266557 IC50 = 2.4 nM 8.62
CHEMBL9406 IC50 = 5.0 nM 8.30
CHEMBL9267 IC50 = 5.0 nM 8.30
CHEMBL275307 IC50 = 5.8 nM 8.24
CHEMBL276627 IC50 = 5.9 nM 8.23
CHEMBL8954 IC50 = 8.0 nM 8.10
CHEMBL9449 IC50 = 8.0 nM 8.10
CHEMBL9534 IC50 = 8.0 nM 8.10
CHEMBL9387 L-365260 IC50 = 8.5 nM 8.07
CHEMBL9026 IC50 = 9.3 nM 8.03
CHEMBL9319 IC50 = 10.0 nM 8.00
CHEMBL266120 IC50 = 11.0 nM 7.96
CHEMBL8997 IC50 = 14.0 nM 7.85
CHEMBL9083 IC50 = 14.0 nM 7.85
CHEMBL9524 IC50 = 14.0 nM 7.85
CHEMBL9422 IC50 = 14.0 nM 7.85
CHEMBL9291 IC50 = 15.0 nM 7.82
CHEMBL9354 IC50 = 15.0 nM 7.82
CHEMBL9459 IC50 = 16.0 nM 7.80
CHEMBL8922 IC50 = 22.0 nM 7.66
CHEMBL9195 IC50 = 23.0 nM 7.64
CHEMBL9311 IC50 = 25.0 nM 7.60
CHEMBL9501 IC50 = 26.0 nM 7.58
CHEMBL267023 IC50 = 29.0 nM 7.54
CHEMBL269123 IC50 = 33.0 nM 7.48
CHEMBL415965 IC50 = 38.0 nM 7.42
CHEMBL9377 IC50 = 45.0 nM 7.35
CHEMBL262569 IC50 = 50.0 nM 7.30
CHEMBL269662 IC50 = 57.0 nM 7.24
CHEMBL9171 IC50 = 63.0 nM 7.20
CHEMBL9287 IC50 = 73.0 nM 7.14
CHEMBL9888 IC50 = 88.0 nM 7.06
CHEMBL9535 IC50 = 97.0 nM 7.01
CHEMBL269606 IC50 = 108.0 nM 6.97
CHEMBL273693 IC50 = 140.0 nM 6.85
CHEMBL9336 IC50 = 152.0 nM 6.82
CHEMBL266376 IC50 = 200.0 nM 6.70
CHEMBL9465 IC50 = 219.0 nM 6.66
CHEMBL269142 IC50 = 225.0 nM 6.65
CHEMBL9492 IC50 = 262.0 nM 6.58
CHEMBL8921 IC50 = 319.0 nM 6.50
CHEMBL8920 IC50 = 592.0 nM 6.23
CHEMBL266598 IC50 = 585.0 nM 6.23
CHEMBL9230 IC50 = 611.0 nM 6.21
CHEMBL266523 IC50 = 915.0 nM 6.04
CHEMBL8905 IC50 = 1083.0 nM 5.96