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Assay Detail

CHEMBL701403

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

Binding
Affinity at K opioid receptor on membranes prepared from guinea pig cerebellum by [3H]- 69593 displacement.
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists
Gottschlich R, Ackermann K, Barber A, Bartoszyk G, Greiner H
Bioorg Med Chem Lett (1994) 4 : 677 -682
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.24 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58033 (-)-U-50488 1 9.00
CHEMBL559010 1 9.00
CHEMBL540342 ASIMADOLINE HYDROCHLORIDE 1 8.70
CHEMBL555800 2 8.52
CHEMBL543707 1 8.40
CHEMBL538802 1 8.40
CHEMBL543236 1 8.40
CHEMBL543476 1 8.30
CHEMBL540345 1 8.22
CHEMBL543947 1 8.22
CHEMBL538063 1 8.22
CHEMBL543948 1 8.22
CHEMBL540335 1 8.15
CHEMBL542036 1 8.15
CHEMBL545346 2 8.00
CHEMBL553085 1 8.00
CHEMBL539317 1 7.70
CHEMBL553084 1 7.70
CHEMBL552587 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58033 (-)-U-50488 Ki = 1.0 nM 9.00
CHEMBL559010 Ki = 1.0 nM 9.00
CHEMBL540342 ASIMADOLINE HYDROCHLORIDE Ki = 2.0 nM 8.70
CHEMBL555800 Ki = 3.0 nM 8.52
CHEMBL543707 Ki = 4.0 nM 8.40
CHEMBL538802 Ki = 4.0 nM 8.40
CHEMBL543236 Ki = 4.0 nM 8.40
CHEMBL543476 Ki = 5.0 nM 8.30
CHEMBL538063 Ki = 6.0 nM 8.22
CHEMBL543947 Ki = 6.0 nM 8.22
CHEMBL540345 Ki = 6.0 nM 8.22
CHEMBL543948 Ki = 6.0 nM 8.22
CHEMBL542036 Ki = 7.0 nM 8.15
CHEMBL540335 Ki = 7.0 nM 8.15
CHEMBL545346 Ki = 10.0 nM 8.00
CHEMBL545346 Ki = 10.0 nM 8.00
CHEMBL555800 Ki = 10.0 nM 8.00
CHEMBL553085 Ki = 10.0 nM 8.00
CHEMBL539317 Ki = 20.0 nM 7.70
CHEMBL552587 Ki = 20.0 nM 7.70
CHEMBL553084 Ki = 20.0 nM 7.70