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Assay Detail

CHEMBL754959

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

Binding
Binding affinity against opioid receptor mu using [3H]-DAMGO as radioligand.
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors.
Carroll FI, Abraham P, Parham K, Bai X, Zhang X, Brine GA, Mascarella SW, Martin BR, May EL, Sauss C.
J Med Chem (1992) 35 : 2812 -2818
PubMed 1322987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.14 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 1 9.74
CHEMBL316632 1 9.70
CHEMBL2367791 1 8.82
CHEMBL2367796 1 8.52
CHEMBL98883 1 8.44
CHEMBL2367800 1 8.40
CHEMBL2367790 1 8.31
CHEMBL2367789 1 8.29
CHEMBL2367797 1 8.23
CHEMBL2367798 1 8.05
CHEMBL2367792 1 7.96
CHEMBL2367794 1 7.96
CHEMBL560 1 7.89
CHEMBL2368630 1 7.70
CHEMBL2367787 1 7.64
CHEMBL94350 1 7.26
CHEMBL2367801 1 7.17
CHEMBL2368614 1 7.01
CHEMBL2367793 1 6.58
CHEMBL2367788 1 6.57
CHEMBL2368631 1 6.46
CHEMBL2367795 1 6.33
CHEMBL2367807 1 6.16
CHEMBL2367809 1 6.00
CHEMBL2021605 1 5.91
CHEMBL2368615 1 5.79
CHEMBL60542 (+)-PENTAZOCINE 1 5.77
CHEMBL2367808 1 5.77
CHEMBL2367804 1 5.70
CHEMBL2367806 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 0.18 nM 9.74
CHEMBL316632 Ki = 0.2 nM 9.70
CHEMBL2367791 Ki = 1.5 nM 8.82
CHEMBL2367796 Ki = 3.0 nM 8.52
CHEMBL98883 Ki = 3.6 nM 8.44
CHEMBL2367800 Ki = 4.0 nM 8.40
CHEMBL2367790 Ki = 4.9 nM 8.31
CHEMBL2367789 Ki = 5.1 nM 8.29
CHEMBL2367797 Ki = 5.9 nM 8.23
CHEMBL2367798 Ki = 9.0 nM 8.05
CHEMBL2367792 Ki = 11.0 nM 7.96
CHEMBL2367794 Ki = 11.0 nM 7.96
CHEMBL560 Ki = 13.0 nM 7.89
CHEMBL2368630 Ki = 20.0 nM 7.70
CHEMBL2367787 Ki = 23.0 nM 7.64
CHEMBL94350 Ki = 55.0 nM 7.26
CHEMBL2367801 Ki = 68.0 nM 7.17
CHEMBL2368614 Ki = 97.0 nM 7.01
CHEMBL2367793 Ki = 260.0 nM 6.58
CHEMBL2367788 Ki = 270.0 nM 6.57
CHEMBL2368631 Ki = 343.0 nM 6.46
CHEMBL2367795 Ki = 470.0 nM 6.33
CHEMBL2367807 Ki = 690.0 nM 6.16
CHEMBL2367809 Ki = 1000.0 nM 6.00
CHEMBL2021605 Ki = 1240.0 nM 5.91
CHEMBL2368615 Ki = 1610.0 nM 5.79
CHEMBL60542 (+)-PENTAZOCINE Ki = 1700.0 nM 5.77
CHEMBL2367808 Ki = 1690.0 nM 5.77
CHEMBL2367804 Ki = 1980.0 nM 5.70
CHEMBL2367806 Ki = 2270.0 nM 5.64
CHEMBL2367802 Ki = 3500.0 nM 5.46
CHEMBL2367803 Ki = 4970.0 nM 5.30
CHEMBL2367799 Ki = 5620.0 nM 5.25
CHEMBL101510 Ki > 10000.0 nM -