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Assay Detail

CHEMBL1674428

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Nemoto T, Yamamoto N, Watanabe A, Fujii H, Hasebe K, Nakajima M, Mochizuki H, Nagase H.
Bioorg Med Chem (2011) 19 : 1205 -1221
PubMed 21256034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 9.26 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672477 1 10.28
CHEMBL1672472 1 10.08
CHEMBL1672470 1 9.96
CHEMBL1672481 1 9.96
CHEMBL1672479 1 9.92
CHEMBL1672473 1 9.92
CHEMBL1672469 1 9.89
CHEMBL1672471 1 9.88
CHEMBL1672475 1 9.87
CHEMBL1672490 1 9.86
CHEMBL1672480 1 9.83
CHEMBL1672468 1 9.81
CHEMBL1672484 1 9.74
CHEMBL1672474 1 9.73
CHEMBL1672483 1 9.61
CHEMBL1672476 1 9.57
CHEMBL1672478 1 9.54
CHEMBL1672486 1 9.41
CHEMBL1672487 1 9.33
CHEMBL267495 NALFURAFINE 4.0 1 9.23
CHEMBL1672485 1 9.02
CHEMBL1672494 1 8.87
CHEMBL1672482 1 8.36
CHEMBL1672491 1 8.21
CHEMBL1672493 1 8.17
CHEMBL1672489 1 7.76
CHEMBL1672492 1 7.74
CHEMBL1672488 1 7.57
CHEMBL573214 NORBINALTORPHIMINE 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672477 Ki = 0.0522 nM 10.28
CHEMBL1672472 Ki = 0.0828 nM 10.08
CHEMBL1672470 Ki = 0.109 nM 9.96
CHEMBL1672481 Ki = 0.11 nM 9.96
CHEMBL1672479 Ki = 0.12 nM 9.92
CHEMBL1672473 Ki = 0.121 nM 9.92
CHEMBL1672469 Ki = 0.129 nM 9.89
CHEMBL1672471 Ki = 0.132 nM 9.88
CHEMBL1672475 Ki = 0.134 nM 9.87
CHEMBL1672490 Ki = 0.138 nM 9.86
CHEMBL1672480 Ki = 0.147 nM 9.83
CHEMBL1672468 Ki = 0.156 nM 9.81
CHEMBL1672484 Ki = 0.182 nM 9.74
CHEMBL1672474 Ki = 0.188 nM 9.73
CHEMBL1672483 Ki = 0.243 nM 9.61
CHEMBL1672476 Ki = 0.27 nM 9.57
CHEMBL1672478 Ki = 0.29 nM 9.54
CHEMBL1672486 Ki = 0.389 nM 9.41
CHEMBL1672487 Ki = 0.466 nM 9.33
CHEMBL267495 NALFURAFINE Ki = 0.582 nM 9.23
CHEMBL1672485 Ki = 0.946 nM 9.02
CHEMBL1672494 Ki = 1.35 nM 8.87
CHEMBL1672482 Ki = 4.38 nM 8.36
CHEMBL1672491 Ki = 6.16 nM 8.21
CHEMBL1672493 Ki = 6.79 nM 8.17
CHEMBL1672489 Ki = 17.4 nM 7.76
CHEMBL1672492 Ki = 18.3 nM 7.74
CHEMBL1672488 Ki = 27.2 nM 7.57
CHEMBL573214 NORBINALTORPHIMINE Ki = 28.2 nM 7.55