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Assay Detail

CHEMBL3376870

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

Binding
Displacement of radioligand from rat KISS1R transfected in CHO cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

KiSS-1 receptor (CHEMBL1169599)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
Asami T, Nishizawa N, Matsui H, Takatsu Y, Suzuki A, Kiba A, Terada M, Nishibori K, Nakayama M, Ban J, Matsumoto S, Tarui N, Ikeda Y, Yamaguchi M, Kusaka M, Ohtaki T, Kitada C.
J Med Chem (2014) 57 : 6105 -6115
PubMed 24918545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 9.77 10.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314224 1 10.16
CHEMBL3314215 1 10.11
CHEMBL3314229 1 10.06
CHEMBL3314226 1 10.06
CHEMBL376756 KISSPEPTIN-10 3.0 1 10.06
CHEMBL3314225 1 9.96
CHEMBL3314207 1 9.89
CHEMBL3086284 KISS1-305 1 9.85
CHEMBL3314228 1 9.77
CHEMBL3314222 1 9.08
CHEMBL3314218 1 8.44
CHEMBL3315315 1 -
CHEMBL3314208 1 -
CHEMBL3314209 1 -
CHEMBL3314210 1 -
CHEMBL3314211 1 -
CHEMBL3314212 1 -
CHEMBL3314213 1 -
CHEMBL3314214 1 -
CHEMBL3314216 1 -
CHEMBL3314219 1 -
CHEMBL3314220 1 -
CHEMBL3314221 1 -
CHEMBL3314223 1 -
CHEMBL3314227 1 -
CHEMBL3314217 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314224 Ki = 0.069 nM 10.16
CHEMBL3314215 Ki = 0.077 nM 10.11
CHEMBL3314229 Ki = 0.087 nM 10.06
CHEMBL3314226 Ki = 0.087 nM 10.06
CHEMBL376756 KISSPEPTIN-10 Ki = 0.088 nM 10.06
CHEMBL3314225 Ki = 0.11 nM 9.96
CHEMBL3314207 Ki = 0.13 nM 9.89
CHEMBL3086284 KISS1-305 Ki = 0.14 nM 9.85
CHEMBL3314228 Ki = 0.17 nM 9.77
CHEMBL3314222 Ki = 0.83 nM 9.08
CHEMBL3314218 Ki = 3.6 nM 8.44
CHEMBL3315315 Ki - -
CHEMBL3314208 Ki - -
CHEMBL3314209 Ki - -
CHEMBL3314210 Ki - -
CHEMBL3314211 Ki - -
CHEMBL3314212 Ki - -
CHEMBL3314213 Ki - -
CHEMBL3314214 Ki - -
CHEMBL3314216 Ki - -
CHEMBL3314219 Ki - -
CHEMBL3314220 Ki - -
CHEMBL3314221 Ki - -
CHEMBL3314223 Ki - -
CHEMBL3314227 Ki - -
CHEMBL3314217 Ki - -