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Assay Detail

CHEMBL1030624

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

Binding
Displacement of [125I]diprenorphine from human KOP expressed in CHO cells
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2.
Caldwell JP, Matasi JJ, Fernandez X, McLeod RL, Zhang H, Fawzi A, Tulshian DB.
Bioorg Med Chem Lett (2009) 19 : 1164 -1167
PubMed 19147350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 6.70 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475310 1 8.10
CHEMBL473700 1 8.00
CHEMBL516187 1 7.96
CHEMBL514662 1 7.89
CHEMBL511161 1 7.85
CHEMBL473904 1 7.82
CHEMBL471880 1 7.60
CHEMBL472669 1 7.60
CHEMBL471882 1 7.58
CHEMBL516389 1 7.54
CHEMBL514463 1 7.48
CHEMBL474687 1 7.41
CHEMBL475707 1 7.40
CHEMBL473272 1 7.35
CHEMBL474092 1 7.35
CHEMBL474485 1 7.32
CHEMBL515091 1 7.31
CHEMBL240215 1 7.28
CHEMBL515142 1 7.27
CHEMBL511649 1 7.25
CHEMBL473701 1 7.25
CHEMBL473279 1 7.19
CHEMBL464191 1 7.19
CHEMBL514489 1 7.17
CHEMBL517167 1 7.17
CHEMBL515575 1 7.09
CHEMBL473280 1 7.07
CHEMBL474096 1 6.86
CHEMBL240657 1 6.86
CHEMBL510201 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475310 Ki = 8.0 nM 8.10
CHEMBL473700 Ki = 10.0 nM 8.00
CHEMBL516187 Ki = 11.0 nM 7.96
CHEMBL514662 Ki = 13.0 nM 7.89
CHEMBL511161 Ki = 14.0 nM 7.85
CHEMBL473904 Ki = 15.0 nM 7.82
CHEMBL471880 Ki = 25.0 nM 7.60
CHEMBL472669 Ki = 25.0 nM 7.60
CHEMBL471882 Ki = 26.0 nM 7.58
CHEMBL516389 Ki = 29.0 nM 7.54
CHEMBL514463 Ki = 33.0 nM 7.48
CHEMBL474687 Ki = 39.0 nM 7.41
CHEMBL475707 Ki = 40.0 nM 7.40
CHEMBL474092 Ki = 45.0 nM 7.35
CHEMBL473272 Ki = 45.0 nM 7.35
CHEMBL474485 Ki = 48.0 nM 7.32
CHEMBL515091 Ki = 49.0 nM 7.31
CHEMBL240215 Ki = 52.0 nM 7.28
CHEMBL515142 Ki = 54.0 nM 7.27
CHEMBL511649 Ki = 56.0 nM 7.25
CHEMBL473701 Ki = 56.0 nM 7.25
CHEMBL473279 Ki = 65.0 nM 7.19
CHEMBL464191 Ki = 64.0 nM 7.19
CHEMBL514489 Ki = 68.0 nM 7.17
CHEMBL517167 Ki = 68.0 nM 7.17
CHEMBL515575 Ki = 82.0 nM 7.09
CHEMBL473280 Ki = 86.0 nM 7.07
CHEMBL474096 Ki = 138.0 nM 6.86
CHEMBL240657 Ki = 137.0 nM 6.86
CHEMBL510201 Ki = 150.0 nM 6.82
CHEMBL511162 Ki = 151.0 nM 6.82
CHEMBL472086 Ki = 158.0 nM 6.80
CHEMBL515829 Ki = 165.0 nM 6.78
CHEMBL473898 Ki = 169.0 nM 6.77
CHEMBL473278 Ki = 174.0 nM 6.76
CHEMBL475094 Ki = 208.0 nM 6.68
CHEMBL510745 Ki = 224.0 nM 6.65
CHEMBL457244 Ki = 238.0 nM 6.62
CHEMBL456225 Ki = 247.0 nM 6.61
CHEMBL457451 Ki = 254.0 nM 6.59
CHEMBL501088 Ki = 271.0 nM 6.57
CHEMBL464192 Ki = 279.0 nM 6.55
CHEMBL460636 Ki = 320.0 nM 6.50
CHEMBL518325 Ki = 469.0 nM 6.33
CHEMBL475096 Ki = 497.0 nM 6.30
CHEMBL474091 Ki = 506.0 nM 6.30
CHEMBL239822 Ki = 540.0 nM 6.27
CHEMBL472676 Ki = 543.0 nM 6.26
CHEMBL472677 Ki = 633.0 nM 6.20
CHEMBL474283 Ki = 655.0 nM 6.18