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Assay Detail

CHEMBL805774

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Binding
Binding affinity against sigma opioid receptor using [3H]pentazocine as radioligand.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 24 7.44 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2368615 1 9.17
CHEMBL2368631 1 8.94
CHEMBL2367802 1 8.65
CHEMBL2367793 1 8.58
CHEMBL60542 (+)-PENTAZOCINE 1 8.51
CHEMBL2367788 1 8.49
CHEMBL94350 1 8.41
CHEMBL2367790 1 8.06
CHEMBL2367804 1 7.98
CHEMBL2021605 1 7.76
CHEMBL2368614 1 7.44
CHEMBL2367801 1 7.42
CHEMBL2368630 1 7.41
CHEMBL101510 1 7.22
CHEMBL316632 1 7.21
CHEMBL560 1 7.08
CHEMBL2367800 1 7.07
CHEMBL2367791 1 6.39
CHEMBL2367803 1 5.68
CHEMBL56585 CYCLAZOCINE 2.0 1 5.58
CHEMBL2367795 1 5.47
CHEMBL2367787 1 5.25
CHEMBL2367794 1 -
CHEMBL98883 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2368615 Ki = 0.67 nM 9.17
CHEMBL2368631 Ki = 1.15 nM 8.94
CHEMBL2367802 Ki = 2.25 nM 8.65
CHEMBL2367793 Ki = 2.64 nM 8.58
CHEMBL60542 (+)-PENTAZOCINE Ki = 3.1 nM 8.51
CHEMBL2367788 Ki = 3.23 nM 8.49
CHEMBL94350 Ki = 3.9 nM 8.41
CHEMBL2367790 Ki = 8.74 nM 8.06
CHEMBL2367804 Ki = 10.5 nM 7.98
CHEMBL2021605 Ki = 17.2 nM 7.76
CHEMBL2368614 Ki = 36.5 nM 7.44
CHEMBL2367801 Ki = 38.5 nM 7.42
CHEMBL2368630 Ki = 38.6 nM 7.41
CHEMBL101510 Ki = 59.7 nM 7.22
CHEMBL316632 Ki = 61.7 nM 7.21
CHEMBL560 Ki = 83.1 nM 7.08
CHEMBL2367800 Ki = 85.2 nM 7.07
CHEMBL2367791 Ki = 403.0 nM 6.39
CHEMBL2367803 Ki = 2100.0 nM 5.68
CHEMBL56585 CYCLAZOCINE Ki = 2650.0 nM 5.58
CHEMBL2367795 Ki = 3380.0 nM 5.47
CHEMBL2367787 Ki = 5580.0 nM 5.25
CHEMBL2367794 Ki > 6000.0 nM -
CHEMBL98883 Ki > 3000.0 nM -