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Assay Detail

CHEMBL663471

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

Binding
Half-maximal inhibition of [125I]-CCK-33 binding to rat pancreas cholecystokinin receptor
ChEMBL ↗
64
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cholecystokinin receptor (CHEMBL2096986) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 64 5.30 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907724 — — 1 7.00
CHEMBL1907717 — — 1 6.57
CHEMBL1907728 — — 1 6.52
CHEMBL1907742 — — 1 6.52
CHEMBL1907731 — — 1 6.52
CHEMBL1907729 — — 1 6.44
CHEMBL1907714 — — 1 6.30
CHEMBL1907720 — — 1 6.16
CHEMBL51569 — — 1 5.92
CHEMBL1907740 — — 1 5.92
CHEMBL20872 — — 1 5.89
CHEMBL430336 — — 1 5.85
CHEMBL1907711 — — 1 5.85
CHEMBL1907719 — — 1 5.85
CHEMBL283117 ASPERLICIN — 1 5.85
CHEMBL1907725 — — 1 5.68
CHEMBL1907737 — — 1 5.66
CHEMBL283946 — — 1 5.54
CHEMBL2092748 — — 1 5.50
CHEMBL70728 — — 1 5.47
CHEMBL1907716 — — 1 5.44
CHEMBL1907738 — — 1 5.40
CHEMBL1907744 — — 1 5.35
CHEMBL20683 — — 1 5.33
CHEMBL1907741 — — 1 5.30
CHEMBL552817 — — 1 5.18
CHEMBL1907730 — — 1 5.08
CHEMBL429063 — — 1 5.00
CHEMBL2092746 — — 2 5.00
CHEMBL1907930 — — 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907724 — IC50 = 100.0 nM 7.00
CHEMBL1907717 — IC50 = 270.0 nM 6.57
CHEMBL1907728 — IC50 = 300.0 nM 6.52
CHEMBL1907742 — IC50 = 300.0 nM 6.52
CHEMBL1907731 — IC50 = 300.0 nM 6.52
CHEMBL1907729 — IC50 = 360.0 nM 6.44
CHEMBL1907714 — IC50 = 500.0 nM 6.30
CHEMBL1907720 — IC50 = 700.0 nM 6.16
CHEMBL1907740 — IC50 = 1200.0 nM 5.92
CHEMBL51569 — IC50 = 1200.0 nM 5.92
CHEMBL20872 — IC50 = 1300.0 nM 5.89
CHEMBL283117 ASPERLICIN IC50 = 1400.0 nM 5.85
CHEMBL430336 — IC50 = 1400.0 nM 5.85
CHEMBL1907719 — IC50 = 1400.0 nM 5.85
CHEMBL1907711 — IC50 = 1400.0 nM 5.85
CHEMBL1907725 — IC50 = 2100.0 nM 5.68
CHEMBL1907737 — IC50 = 2200.0 nM 5.66
CHEMBL283946 — IC50 = 2900.0 nM 5.54
CHEMBL2092748 — IC50 = 3200.0 nM 5.50
CHEMBL70728 — IC50 = 3400.0 nM 5.47
CHEMBL1907716 — IC50 = 3600.0 nM 5.44
CHEMBL1907738 — IC50 = 4000.0 nM 5.40
CHEMBL1907744 — IC50 = 4500.0 nM 5.35
CHEMBL20683 — IC50 = 4700.0 nM 5.33
CHEMBL1907741 — IC50 = 5000.0 nM 5.30
CHEMBL552817 — IC50 = 6600.0 nM 5.18
CHEMBL1907730 — IC50 = 8300.0 nM 5.08
CHEMBL2092746 — IC50 = 10000.0 nM 5.00
CHEMBL429063 — IC50 = 10000.0 nM 5.00
CHEMBL1907930 — IC50 = 10600.0 nM 4.97
CHEMBL2092988 — IC50 = 11000.0 nM 4.96
CHEMBL2092991 — IC50 = 11000.0 nM 4.96
CHEMBL1907721 — IC50 = 11000.0 nM 4.96
CHEMBL1907726 — IC50 = 12000.0 nM 4.92
CHEMBL2092990 — IC50 = 13000.0 nM 4.89
CHEMBL2092749 — IC50 = 17000.0 nM 4.77
CHEMBL1907735 — IC50 = 18000.0 nM 4.75
CHEMBL3350230 — IC50 = 21000.0 nM 4.68
CHEMBL2092989 — IC50 = 21000.0 nM 4.68
CHEMBL429391 — IC50 = 23000.0 nM 4.64
CHEMBL1907723 — IC50 = 24000.0 nM 4.62
CHEMBL20223 — IC50 = 25000.0 nM 4.60
CHEMBL1907931 — IC50 = 32000.0 nM 4.50
CHEMBL20408 — IC50 = 33000.0 nM 4.48
CHEMBL1907736 — IC50 = 42000.0 nM 4.38
CHEMBL1907739 — IC50 = 48000.0 nM 4.32
CHEMBL20514 — IC50 = 49000.0 nM 4.31
CHEMBL1907734 — IC50 = 60000.0 nM 4.22
CHEMBL1907712 — IC50 = 80000.0 nM 4.10
CHEMBL279237 — IC50 = 100000.0 nM 4.00