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Assay Detail

CHEMBL749722

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

Binding
Binding affinity towards Mutant D216N, D217N, E218Q Opioid receptor kappa 1 EL-2 expressed in HEK cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
Ferguson DM, Kramer S, Metzger TG, Law PY, Portoghese PS.
J Med Chem (2000) 43 : 1251 -1252
PubMed 10753461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.59 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440765 U-69593 1 8.70
CHEMBL405618 ANALOG OF DYNORPHIN A 1 8.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440765 U-69593 Ki = 2.0 nM 8.70
CHEMBL405618 ANALOG OF DYNORPHIN A Ki = 3.4 nM 8.47