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Assay Detail

CHEMBL2387944

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

Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effect of anchoring 4-anilidopiperidines to opioid peptides.
Petrov RR, Lee YS, Vardanyan RS, Liu L, Ma SW, Davis P, Lai J, Porreca F, Vanderah TW, Hruby VJ.
Bioorg Med Chem Lett (2013) 23 : 3434 -3437
PubMed 23623418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.65 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2387214 1 9.59
CHEMBL2387211 1 9.55
CHEMBL2387327 1 9.46
CHEMBL2387328 1 9.29
CHEMBL2387329 1 9.20
CHEMBL214022 1 9.00
CHEMBL2387337 1 8.96
CHEMBL20226 DELTORPHIN II 1 8.89
CHEMBL2387215 1 8.74
CHEMBL200199 BIPHALIN 1 8.59
CHEMBL2387339 1 8.55
CHEMBL405618 ANALOG OF DYNORPHIN A 1 8.42
CHEMBL2387210 1 8.40
CHEMBL2387216 1 8.34
CHEMBL2387213 1 7.96
CHEMBL2387338 1 7.92
CHEMBL2387212 1 7.62
CHEMBL2387341 1 7.57
CHEMBL2387330 1 7.08
CHEMBL2387331 1 6.23
CHEMBL2387340 1 6.20
CHEMBL2387332 1 6.00
CHEMBL2387336 1 5.34
CHEMBL316446 ENDOMORPHIN-1 1 5.29
CHEMBL216492 1 5.12
CHEMBL2387334 1 4.89
CHEMBL2387335 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2387214 Ki = 0.26 nM 9.59
CHEMBL2387211 Ki = 0.28 nM 9.55
CHEMBL2387327 Ki = 0.35 nM 9.46
CHEMBL2387328 Ki = 0.51 nM 9.29
CHEMBL2387329 Ki = 0.63 nM 9.20
CHEMBL214022 Ki = 0.99 nM 9.00
CHEMBL2387337 Ki = 1.1 nM 8.96
CHEMBL20226 DELTORPHIN II Ki = 1.3 nM 8.89
CHEMBL2387215 Ki = 1.8 nM 8.74
CHEMBL200199 BIPHALIN Ki = 2.6 nM 8.59
CHEMBL2387339 Ki = 2.8 nM 8.55
CHEMBL405618 ANALOG OF DYNORPHIN A Ki = 3.8 nM 8.42
CHEMBL2387210 Ki = 4.0 nM 8.40
CHEMBL2387216 Ki = 4.6 nM 8.34
CHEMBL2387213 Ki = 11.0 nM 7.96
CHEMBL2387338 Ki = 12.0 nM 7.92
CHEMBL2387212 Ki = 24.0 nM 7.62
CHEMBL2387341 Ki = 27.0 nM 7.57
CHEMBL2387330 Ki = 84.0 nM 7.08
CHEMBL2387331 Ki = 590.0 nM 6.23
CHEMBL2387340 Ki = 630.0 nM 6.20
CHEMBL2387332 Ki = 1000.0 nM 6.00
CHEMBL2387336 Ki = 4600.0 nM 5.34
CHEMBL316446 ENDOMORPHIN-1 Ki = 5100.0 nM 5.29
CHEMBL216492 Ki = 7600.0 nM 5.12
CHEMBL2387334 Ki = 13000.0 nM 4.89
CHEMBL2387335 Ki = 36000.0 nM 4.44