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Assay Detail

CHEMBL863863

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in rat brain
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of potent phenyl imidazoles as opioid receptor agonists.
Breslin HJ, Cai C, Miskowski TA, Coutinho SV, Zhang SP, Hornby P, He W.
Bioorg Med Chem Lett (2006) 16 : 2505 -2508
PubMed 16483774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.30 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377069 1 10.30
CHEMBL205049 1 9.89
CHEMBL208454 1 9.52
CHEMBL208461 1 9.52
CHEMBL204996 1 8.92
CHEMBL427214 1 8.85
CHEMBL366311 1 8.82
CHEMBL383197 1 8.42
CHEMBL208164 1 7.75
CHEMBL361033 1 7.68
CHEMBL205388 1 7.64
CHEMBL361274 1 7.26
CHEMBL440221 1 6.75
CHEMBL205533 1 6.68
CHEMBL205273 1 6.45
CHEMBL207976 1 6.38
CHEMBL383456 1 6.35
CHEMBL206660 1 6.23
CHEMBL208400 1 6.07
CHEMBL206888 1 6.04
CHEMBL205329 1 5.88
CHEMBL381728 1 5.74
CHEMBL205281 1 5.28
CHEMBL207743 1 5.24
CHEMBL381793 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377069 Ki = 0.05 nM 10.30
CHEMBL205049 Ki = 0.13 nM 9.89
CHEMBL208454 Ki = 0.3 nM 9.52
CHEMBL208461 Ki = 0.3 nM 9.52
CHEMBL204996 Ki = 1.2 nM 8.92
CHEMBL427214 Ki = 1.4 nM 8.85
CHEMBL366311 Ki = 1.5 nM 8.82
CHEMBL383197 Ki = 3.8 nM 8.42
CHEMBL208164 Ki = 18.0 nM 7.75
CHEMBL361033 Ki = 21.0 nM 7.68
CHEMBL205388 Ki = 23.0 nM 7.64
CHEMBL361274 Ki = 55.0 nM 7.26
CHEMBL440221 Ki = 179.0 nM 6.75
CHEMBL205533 Ki = 207.0 nM 6.68
CHEMBL205273 Ki = 356.0 nM 6.45
CHEMBL207976 Ki = 413.0 nM 6.38
CHEMBL383456 Ki = 443.0 nM 6.35
CHEMBL206660 Ki = 592.0 nM 6.23
CHEMBL208400 Ki = 857.0 nM 6.07
CHEMBL206888 Ki = 912.0 nM 6.04
CHEMBL205329 Ki = 1335.0 nM 5.88
CHEMBL381728 Ki = 1835.0 nM 5.74
CHEMBL205281 Ki = 5260.0 nM 5.28
CHEMBL207743 Ki = 5800.0 nM 5.24
CHEMBL381793 Ki = 12800.0 nM 4.89