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Assay Detail

CHEMBL751670

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Binding
Affinity of [H]DADLE to the delta 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

Delta-type opioid receptor (CHEMBL269)
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 7.53 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 9.04
CHEMBL13470 SNC-80 1 8.80
CHEMBL174894 1 8.73
CHEMBL2112954 1 8.70
CHEMBL2112960 2 8.56
CHEMBL22650 3 8.25
CHEMBL353745 1 7.82
CHEMBL2112953 1 7.75
CHEMBL607014 1 7.73
CHEMBL368861 1 7.70
CHEMBL176037 1 7.66
CHEMBL174569 1 7.44
CHEMBL176806 1 7.44
CHEMBL177610 1 7.44
CHEMBL368835 1 7.34
CHEMBL607015 1 7.28
CHEMBL175511 1 7.17
CHEMBL434685 1 7.14
CHEMBL607064 1 7.03
CHEMBL355580 1 7.03
CHEMBL178895 1 6.90
CHEMBL607065 1 6.85
CHEMBL607066 1 6.75
CHEMBL172971 1 6.71
CHEMBL175342 1 6.64
CHEMBL174533 1 6.59
CHEMBL177720 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 Ki = 0.91 nM 9.04
CHEMBL13470 SNC-80 Ki = 1.57 nM 8.80
CHEMBL174894 Ki = 1.85 nM 8.73
CHEMBL2112954 Ki = 2.0 nM 8.70
CHEMBL2112960 Ki = 2.72 nM 8.56
CHEMBL22650 Ki = 5.58 nM 8.25
CHEMBL2112960 Ki = 7.0 nM 8.15
CHEMBL22650 Ki = 11.9 nM 7.92
CHEMBL353745 Ki = 15.0 nM 7.82
CHEMBL2112953 Ki = 18.0 nM 7.75
CHEMBL607014 Ki = 18.8 nM 7.73
CHEMBL368861 Ki = 20.0 nM 7.70
CHEMBL176037 Ki = 22.0 nM 7.66
CHEMBL174569 Ki = 36.0 nM 7.44
CHEMBL176806 Ki = 36.0 nM 7.44
CHEMBL177610 Ki = 36.0 nM 7.44
CHEMBL368835 Ki = 45.6 nM 7.34
CHEMBL607015 Ki = 53.0 nM 7.28
CHEMBL175511 Ki = 68.0 nM 7.17
CHEMBL434685 Ki = 72.0 nM 7.14
CHEMBL607064 Ki = 93.0 nM 7.03
CHEMBL355580 Ki = 93.0 nM 7.03
CHEMBL178895 Ki = 126.0 nM 6.90
CHEMBL22650 Ki = 139.0 nM 6.86
CHEMBL607065 Ki = 141.0 nM 6.85
CHEMBL607066 Ki = 178.0 nM 6.75
CHEMBL172971 Ki = 193.0 nM 6.71
CHEMBL175342 Ki = 230.0 nM 6.64
CHEMBL174533 Ki = 257.0 nM 6.59
CHEMBL177720 Ki = 379.0 nM 6.42