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Assay Detail

CHEMBL687331

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

Functional
Half-maximal inhibition of binding of [125I]gastrin to guinea pig gastric glands
58
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Stomach
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
Evans BE, Rittle KE, Bock MG, DiPardo RM, Freidinger RM, Whitter WL, Gould NP, Lundell GF, Homnick CF, Veber DF.
J Med Chem (1987) 30 : 1229 -1239
PubMed 2885419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 4.60 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907728 1 5.30
CHEMBL1907719 1 5.24
CHEMBL51569 1 4.92
CHEMBL1907717 1 4.89
CHEMBL1907720 1 4.89
CHEMBL1907734 1 4.89
CHEMBL429063 1 4.85
CHEMBL20408 1 4.85
CHEMBL2092989 1 4.75
CHEMBL1907731 1 4.68
CHEMBL1907743 1 4.64
CHEMBL1907735 1 4.62
CHEMBL1907733 1 4.60
CHEMBL1907730 1 4.60
CHEMBL1907738 1 4.55
CHEMBL70728 1 4.52
CHEMBL1907736 1 4.42
CHEMBL1907714 1 4.40
CHEMBL1907729 1 4.31
CHEMBL1907740 1 4.30
CHEMBL1907737 1 4.24
CHEMBL1907724 1 4.17
CHEMBL1907931 1 4.16
CHEMBL1907739 1 4.10
CHEMBL2092748 1 4.00
CHEMBL1907721 1 -
CHEMBL1907742 1 -
CHEMBL2092990 1 -
CHEMBL1907718 1 -
CHEMBL20223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907728 IC50 = 5000.0 nM 5.30
CHEMBL1907719 IC50 = 5800.0 nM 5.24
CHEMBL51569 IC50 = 12000.0 nM 4.92
CHEMBL1907717 IC50 = 13000.0 nM 4.89
CHEMBL1907720 IC50 = 13000.0 nM 4.89
CHEMBL1907734 IC50 = 13000.0 nM 4.89
CHEMBL20408 IC50 = 14000.0 nM 4.85
CHEMBL429063 IC50 = 14000.0 nM 4.85
CHEMBL2092989 IC50 = 18000.0 nM 4.75
CHEMBL1907731 IC50 = 21000.0 nM 4.68
CHEMBL1907743 IC50 = 23000.0 nM 4.64
CHEMBL1907735 IC50 = 24000.0 nM 4.62
CHEMBL1907733 IC50 = 25000.0 nM 4.60
CHEMBL1907730 IC50 = 25000.0 nM 4.60
CHEMBL1907738 IC50 = 28000.0 nM 4.55
CHEMBL70728 IC50 = 30000.0 nM 4.52
CHEMBL1907736 IC50 = 38000.0 nM 4.42
CHEMBL1907714 IC50 = 40000.0 nM 4.40
CHEMBL1907729 IC50 = 49000.0 nM 4.31
CHEMBL1907740 IC50 = 50000.0 nM 4.30
CHEMBL1907737 IC50 = 58000.0 nM 4.24
CHEMBL1907724 IC50 = 67000.0 nM 4.17
CHEMBL1907931 IC50 = 70000.0 nM 4.16
CHEMBL1907739 IC50 = 80000.0 nM 4.10
CHEMBL2092748 IC50 = 100000.0 nM 4.00
CHEMBL2092988 IC50 > 100000.0 nM -
CHEMBL1907932 IC50 > 100000.0 nM -
CHEMBL21770 IC50 > 100000.0 nM -
CHEMBL279237 IC50 > 100000.0 nM -
CHEMBL1907930 IC50 > 100000.0 nM -
CHEMBL430336 IC50 > 100000.0 nM -
CHEMBL2092746 IC50 > 100000.0 nM -
CHEMBL1907929 IC50 > 100000.0 nM -
CHEMBL1907715 IC50 > 100000.0 nM -
CHEMBL1907722 IC50 > 100000.0 nM -
CHEMBL1907732 IC50 > 100000.0 nM -
CHEMBL2092746 IC50 > 150000.0 nM -
CHEMBL1907727 IC50 > 100000.0 nM -
CHEMBL1907741 IC50 > 100000.0 nM -
CHEMBL1907718 IC50 > 100000.0 nM -
CHEMBL1907721 IC50 > 100000.0 nM -
CHEMBL1907716 IC50 > 100000.0 nM -
CHEMBL1907742 IC50 > 100000.0 nM -
CHEMBL20872 IC50 > 100000.0 nM -
CHEMBL2092990 IC50 = 140000.0 nM -
CHEMBL20223 IC50 > 100000.0 nM -
CHEMBL3350230 IC50 > 100000.0 nM -
CHEMBL552817 IC50 > 100000.0 nM -
CHEMBL20683 IC50 = 130000.0 nM -
CHEMBL1907723 IC50 > 100000.0 nM -