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Assay Detail

CHEMBL2167536

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

Binding
Displacement of [125I]-BNtxA from mouse cloned MOR-1 expressed in CHO cell membrane after 90 mins
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associated μ opioid receptor (MOR-1) splice variants.
Majumdar S, Subrath J, Le Rouzic V, Polikar L, Burgman M, Nagakura K, Ocampo J, Haselton N, Pasternak AR, Grinnell S, Pan YX, Pasternak GW.
J Med Chem (2012) 55 : 6352 -6362
PubMed 22734622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 8.94 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163536 1 9.96
CHEMBL1795711 1 9.96
CHEMBL2163543 1 9.74
CHEMBL1795712 1 9.66
CHEMBL2163546 1 9.64
CHEMBL2163541 1 9.54
CHEMBL2163544 1 9.37
CHEMBL2163537 1 9.33
CHEMBL2164301 1 9.21
CHEMBL2164296 1 9.18
CHEMBL2164297 1 9.13
CHEMBL2163542 1 9.07
CHEMBL2164298 1 9.02
CHEMBL1795713 1 9.01
CHEMBL2163538 1 8.94
CHEMBL2164295 1 8.85
CHEMBL2163535 1 8.81
CHEMBL2163539 1 8.41
CHEMBL2163540 1 8.39
CHEMBL2163534 1 8.29
CHEMBL2163532 1 8.19
CHEMBL2163545 1 8.19
CHEMBL2164300 1 8.02
CHEMBL2163531 1 7.94
CHEMBL2164299 1 7.69
CHEMBL2163533 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163536 Ki = 0.11 nM 9.96
CHEMBL1795711 Ki = 0.11 nM 9.96
CHEMBL2163543 Ki = 0.18 nM 9.74
CHEMBL1795712 Ki = 0.22 nM 9.66
CHEMBL2163546 Ki = 0.23 nM 9.64
CHEMBL2163541 Ki = 0.29 nM 9.54
CHEMBL2163544 Ki = 0.43 nM 9.37
CHEMBL2163537 Ki = 0.47 nM 9.33
CHEMBL2164301 Ki = 0.61 nM 9.21
CHEMBL2164296 Ki = 0.66 nM 9.18
CHEMBL2164297 Ki = 0.74 nM 9.13
CHEMBL2163542 Ki = 0.85 nM 9.07
CHEMBL2164298 Ki = 0.95 nM 9.02
CHEMBL1795713 Ki = 0.97 nM 9.01
CHEMBL2163538 Ki = 1.15 nM 8.94
CHEMBL2164295 Ki = 1.41 nM 8.85
CHEMBL2163535 Ki = 1.56 nM 8.81
CHEMBL2163539 Ki = 3.85 nM 8.41
CHEMBL2163540 Ki = 4.03 nM 8.39
CHEMBL2163534 Ki = 5.07 nM 8.29
CHEMBL2163532 Ki = 6.5 nM 8.19
CHEMBL2163545 Ki = 6.4 nM 8.19
CHEMBL2164300 Ki = 9.5 nM 8.02
CHEMBL2163531 Ki = 11.54 nM 7.94
CHEMBL2164299 Ki = 20.46 nM 7.69
CHEMBL2163533 Ki > 100.0 nM -