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Assay Detail

CHEMBL873928

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

Binding
mu-2 receptor binding affinity in rat brain by 3H [d-Ala2, (N-Me)Phe4, Gly5-ol] enkephalin displacement.
18
Total Activities
18
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

Structure-activity relationships of some opiate glycosides.
Stachulski AV, Scheinmann F, Ferguson JR, Law JL, Lumbard KW, Hopkins P, Patel N, Clarke S, Gloyne A, Joel SP.
Bioorg Med Chem Lett (2003) 13 : 1207 -1214
PubMed 12643945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.49 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112797 1 8.60
CHEMBL2079659 1 8.49
CHEMBL2112840 1 8.46
CHEMBL2092968 1 8.32
CHEMBL70 MORPHINE 4.0 1 8.32
CHEMBL2112839 1 8.24
CHEMBL19416 1 8.21
CHEMBL3085267 1 8.00
CHEMBL1330 MORPHINE GLUCURONIDE 2.0 1 7.58
CHEMBL3085261 1 7.43
CHEMBL2113393 1 7.36
CHEMBL19396 1 7.32
CHEMBL2079576 1 7.24
CHEMBL440787 1 6.78
CHEMBL2112316 1 6.76
CHEMBL280206 1 6.75
CHEMBL3085275 1 5.79
CHEMBL3085260 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112797 Ki = 2.5 nM 8.60
CHEMBL2079659 Ki = 3.2 nM 8.49
CHEMBL2112840 Ki = 3.5 nM 8.46
CHEMBL2092968 Ki = 4.8 nM 8.32
CHEMBL70 MORPHINE Ki = 4.8 nM 8.32
CHEMBL2112839 Ki = 5.7 nM 8.24
CHEMBL19416 Ki = 6.2 nM 8.21
CHEMBL3085267 Ki = 10.0 nM 8.00
CHEMBL1330 MORPHINE GLUCURONIDE Ki = 26.0 nM 7.58
CHEMBL3085261 Ki = 37.0 nM 7.43
CHEMBL2113393 Ki = 44.0 nM 7.36
CHEMBL19396 Ki = 48.0 nM 7.32
CHEMBL2079576 Ki = 57.0 nM 7.24
CHEMBL440787 Ki = 168.0 nM 6.78
CHEMBL2112316 Ki = 172.0 nM 6.76
CHEMBL280206 Ki = 178.0 nM 6.75
CHEMBL3085275 Ki = 1622.0 nM 5.79
CHEMBL3085260 Ki = 5702.0 nM 5.24