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Assay Detail

CHEMBL758048

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

Binding
Affinity of [3H]DAMGO to the mu opioid receptor from rat brain
30
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
Thomas JB, Herault XM, Rothman RB, Atkinson RN, Burgess JP, Mascarella SW, Dersch CM, Xu H, Flippen-Anderson JL, George CF, Carroll FI.
J Med Chem (2001) 44 : 972 -987
PubMed 11300879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 5.86 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 7.44
CHEMBL2112954 1 7.39
CHEMBL174894 1 6.90
CHEMBL368861 1 6.80
CHEMBL607014 1 6.77
CHEMBL368835 1 6.41
CHEMBL2112960 2 6.03
CHEMBL22650 3 5.92
CHEMBL176806 1 5.90
CHEMBL174533 1 5.82
CHEMBL178895 1 5.80
CHEMBL13470 SNC-80 1 5.79
CHEMBL2112953 1 5.49
CHEMBL607066 1 5.48
CHEMBL177610 1 5.47
CHEMBL353745 1 5.42
CHEMBL607015 1 5.41
CHEMBL177720 1 5.31
CHEMBL172971 1 5.27
CHEMBL176037 1 5.27
CHEMBL434685 1 5.25
CHEMBL175511 1 5.19
CHEMBL607064 1 5.00
CHEMBL175342 1 -
CHEMBL607065 1 -
CHEMBL174569 1 -
CHEMBL355580 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 Ki = 36.0 nM 7.44
CHEMBL2112954 Ki = 40.8 nM 7.39
CHEMBL174894 Ki = 126.0 nM 6.90
CHEMBL368861 Ki = 160.0 nM 6.80
CHEMBL607014 Ki = 171.0 nM 6.77
CHEMBL368835 Ki = 388.0 nM 6.41
CHEMBL2112960 Ki = 938.0 nM 6.03
CHEMBL22650 Ki = 1212.0 nM 5.92
CHEMBL176806 Ki = 1260.0 nM 5.90
CHEMBL174533 Ki = 1511.0 nM 5.82
CHEMBL178895 Ki = 1589.0 nM 5.80
CHEMBL13470 SNC-80 Ki = 1614.0 nM 5.79
CHEMBL22650 Ki = 2623.0 nM 5.58
CHEMBL2112953 Ki = 3252.0 nM 5.49
CHEMBL607066 Ki = 3322.0 nM 5.48
CHEMBL177610 Ki = 3387.0 nM 5.47
CHEMBL2112960 Ki = 3590.0 nM 5.45
CHEMBL353745 Ki = 3785.0 nM 5.42
CHEMBL607015 Ki = 3895.0 nM 5.41
CHEMBL177720 Ki = 4872.0 nM 5.31
CHEMBL172971 Ki = 5341.0 nM 5.27
CHEMBL176037 Ki = 5330.0 nM 5.27
CHEMBL434685 Ki = 5685.0 nM 5.25
CHEMBL175511 Ki = 6425.0 nM 5.19
CHEMBL607064 Ki = 9905.0 nM 5.00
CHEMBL174569 Ki > 6536.0 nM -
CHEMBL22650 Ki > 4854.0 nM -
CHEMBL355580 Ki > 6536.0 nM -
CHEMBL607065 Ki > 5917.0 nM -
CHEMBL175342 Ki > 6536.0 nM -