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Assay Detail

CHEMBL759228

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

Binding
Inhibition of binding of [3H]DAMGO to opioid receptor mu 1 from rat brain membrane.
30
Total Activities
30
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

Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.
Nortey SO, Baxter EW, Codd EE, Zhang SP, Reitz AB.
Bioorg Med Chem Lett (2001) 11 : 1741 -1743
PubMed 11425550 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 6.04 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 8.74
CHEMBL295618 1 6.71
CHEMBL45877 1 6.63
CHEMBL49741 1 6.40
CHEMBL49347 1 6.21
CHEMBL49463 1 6.00
CHEMBL48852 1 6.00
CHEMBL298343 1 6.00
CHEMBL301516 1 5.92
CHEMBL13470 SNC-80 1 5.89
CHEMBL51539 1 5.68
CHEMBL47001 1 5.53
CHEMBL48883 1 5.41
CHEMBL48932 1 5.41
CHEMBL48983 1 5.12
CHEMBL48476 1 5.02
CHEMBL48590 1 -
CHEMBL297574 1 -
CHEMBL49144 1 -
CHEMBL297498 1 -
CHEMBL49712 1 -
CHEMBL48785 1 -
CHEMBL51473 1 -
CHEMBL48417 1 -
CHEMBL48325 1 -
CHEMBL49660 1 -
CHEMBL301587 1 -
CHEMBL46031 1 -
CHEMBL300057 1 -
CHEMBL48542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE Ki = 1.8 nM 8.74
CHEMBL295618 Ki = 197.0 nM 6.71
CHEMBL45877 Ki = 232.0 nM 6.63
CHEMBL49741 Ki = 396.0 nM 6.40
CHEMBL49347 Ki = 618.0 nM 6.21
CHEMBL49463 Ki = 1000.0 nM 6.00
CHEMBL48852 Ki = 1000.0 nM 6.00
CHEMBL298343 Ki = 1000.0 nM 6.00
CHEMBL301516 Ki = 1200.0 nM 5.92
CHEMBL13470 SNC-80 Ki = 1300.0 nM 5.89
CHEMBL51539 Ki = 2070.0 nM 5.68
CHEMBL47001 Ki = 2960.0 nM 5.53
CHEMBL48883 Ki = 3910.0 nM 5.41
CHEMBL48932 Ki = 3930.0 nM 5.41
CHEMBL48983 Ki = 7600.0 nM 5.12
CHEMBL48476 Ki = 9530.0 nM 5.02
CHEMBL48590 Ki > 1000.0 nM -
CHEMBL297574 Ki > 10000.0 nM -
CHEMBL49144 Ki > 10000.0 nM -
CHEMBL297498 Ki > 10000.0 nM -
CHEMBL49712 Ki > 10000.0 nM -
CHEMBL48785 Ki > 10000.0 nM -
CHEMBL51473 Ki > 10000.0 nM -
CHEMBL48417 Ki > 10000.0 nM -
CHEMBL48325 Ki > 10000.0 nM -
CHEMBL49660 Ki > 1000.0 nM -
CHEMBL301587 Ki > 1000.0 nM -
CHEMBL46031 Ki > 1000.0 nM -
CHEMBL300057 Ki > 10000.0 nM -
CHEMBL48542 Ki > 1000.0 nM -