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Assay Detail

CHEMBL993480

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

Functional
Agonist activity at kappa opioid receptor in ddy mouse vas deferens assessed as inhibition of electric stimulation-induced contraction
ChEMBL ↗
36
Total Activities
36
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL4329) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
Kawai K, Hayakawa J, Miyamoto T, Imamura Y, Yamane S, Wakita H, Fujii H, Kawamura K, Matsuura H, Izumimoto N, Kobayashi R, Endo T, Nagase H.
Bioorg Med Chem (2008) 16 : 9188 -9201
PubMed 18829333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 9.03 10.72
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489866 — — 1 10.72
CHEMBL483566 — — 1 10.46
CHEMBL519367 — — 1 10.31
CHEMBL453495 — — 1 10.15
CHEMBL485428 — — 1 10.00
CHEMBL485599 — — 1 10.00
CHEMBL491868 — — 1 9.78
CHEMBL449561 — — 1 9.64
CHEMBL492073 — — 1 9.49
CHEMBL491075 — — 1 9.40
CHEMBL490665 NALFURAFINE HYDROCHLORIDE 4.0 1 9.38
CHEMBL490666 — — 1 9.38
CHEMBL458089 — — 1 9.34
CHEMBL503928 — — 1 9.33
CHEMBL485605 — — 1 9.26
CHEMBL459979 — — 1 9.19
CHEMBL491869 — — 1 9.12
CHEMBL484582 — — 1 9.06
CHEMBL522142 — — 1 8.80
CHEMBL457735 — — 1 8.70
CHEMBL290543 — — 1 8.63
CHEMBL459978 — — 1 7.82
CHEMBL458971 — — 1 7.80
CHEMBL523151 — — 1 7.77
CHEMBL456659 — — 1 7.60
CHEMBL485583 — — 1 7.57
CHEMBL485554 — — 1 7.26
CHEMBL70 MORPHINE 4.0 1 6.84
CHEMBL499774 — — 1 -
CHEMBL502760 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489866 — IC50 = 0.019 nM 10.72
CHEMBL483566 — IC50 = 0.035 nM 10.46
CHEMBL519367 — IC50 = 0.049 nM 10.31
CHEMBL453495 — IC50 = 0.07 nM 10.15
CHEMBL485428 — IC50 = 0.1 nM 10.00
CHEMBL485599 — IC50 = 0.1 nM 10.00
CHEMBL491868 — IC50 = 0.166 nM 9.78
CHEMBL449561 — IC50 = 0.23 nM 9.64
CHEMBL492073 — IC50 = 0.32 nM 9.49
CHEMBL491075 — IC50 = 0.4 nM 9.40
CHEMBL490665 NALFURAFINE HYDROCHLORIDE IC50 = 0.42 nM 9.38
CHEMBL490666 — IC50 = 0.42 nM 9.38
CHEMBL458089 — IC50 = 0.457 nM 9.34
CHEMBL503928 — IC50 = 0.47 nM 9.33
CHEMBL485605 — IC50 = 0.55 nM 9.26
CHEMBL459979 — IC50 = 0.647 nM 9.19
CHEMBL491869 — IC50 = 0.75 nM 9.12
CHEMBL484582 — IC50 = 0.869 nM 9.06
CHEMBL522142 — IC50 = 1.6 nM 8.80
CHEMBL457735 — IC50 = 2.0 nM 8.70
CHEMBL290543 — IC50 = 2.35 nM 8.63
CHEMBL459978 — IC50 = 15.0 nM 7.82
CHEMBL458971 — IC50 = 16.0 nM 7.80
CHEMBL523151 — IC50 = 17.0 nM 7.77
CHEMBL456659 — IC50 = 25.0 nM 7.60
CHEMBL485583 — IC50 = 27.2 nM 7.57
CHEMBL485554 — IC50 = 55.0 nM 7.26
CHEMBL70 MORPHINE IC50 = 145.1 nM 6.84
CHEMBL499774 — IC50 - — -
CHEMBL502760 — IC50 - — -
CHEMBL523093 — IC50 - — -
CHEMBL520991 — IC50 - — -
CHEMBL483376 — IC50 - — -
CHEMBL485437 — IC50 - — -
CHEMBL489057 — IC50 - — -
CHEMBL458819 — Activity - — -