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Assay Detail

CHEMBL3088609

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

Binding
Binding affinity to rat KISS1R
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
Asami T, Nishizawa N, Matsui H, Nishibori K, Ishibashi Y, Horikoshi Y, Nakayama M, Matsumoto S, Tarui N, Yamaguchi M, Matsumoto H, Ohtaki T, Kitada C.
J Med Chem (2013) 56 : 8298 -8307
PubMed 24047141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 9.95 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087793 1 10.40
CHEMBL3087925 1 10.38
CHEMBL3087927 1 10.37
CHEMBL3086282 1 10.29
CHEMBL376756 KISSPEPTIN-10 3.0 1 10.24
CHEMBL3085809 1 10.23
CHEMBL2151646 1 10.17
CHEMBL3085804 1 10.15
CHEMBL3087929 1 10.12
CHEMBL2151654 1 10.04
CHEMBL3087926 1 10.03
CHEMBL3087931 1 10.02
CHEMBL3086284 KISS1-305 1 10.00
CHEMBL2151642 1 9.96
CHEMBL3086283 1 9.96
CHEMBL2151652 1 9.92
CHEMBL2151655 1 9.92
CHEMBL3087928 1 9.92
CHEMBL3086280 1 9.89
CHEMBL3086286 1 9.89
CHEMBL3085806 1 9.85
CHEMBL3086281 1 9.82
CHEMBL3085808 1 9.80
CHEMBL3085807 1 9.74
CHEMBL3085811 1 9.62
CHEMBL3087930 1 9.60
CHEMBL3086285 1 9.55
CHEMBL3085810 1 9.52
CHEMBL3085805 1 9.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087793 Ki = 0.04 nM 10.40
CHEMBL3087925 Ki = 0.042 nM 10.38
CHEMBL3087927 Ki = 0.043 nM 10.37
CHEMBL3086282 Ki = 0.051 nM 10.29
CHEMBL376756 KISSPEPTIN-10 Ki = 0.057 nM 10.24
CHEMBL3085809 Ki = 0.059 nM 10.23
CHEMBL2151646 Ki = 0.068 nM 10.17
CHEMBL3085804 Ki = 0.07 nM 10.15
CHEMBL3087929 Ki = 0.076 nM 10.12
CHEMBL2151654 Ki = 0.092 nM 10.04
CHEMBL3087926 Ki = 0.093 nM 10.03
CHEMBL3087931 Ki = 0.095 nM 10.02
CHEMBL3086284 KISS1-305 Ki = 0.1 nM 10.00
CHEMBL2151642 Ki = 0.11 nM 9.96
CHEMBL3086283 Ki = 0.11 nM 9.96
CHEMBL2151652 Ki = 0.12 nM 9.92
CHEMBL2151655 Ki = 0.12 nM 9.92
CHEMBL3087928 Ki = 0.12 nM 9.92
CHEMBL3086280 Ki = 0.13 nM 9.89
CHEMBL3086286 Ki = 0.13 nM 9.89
CHEMBL3085806 Ki = 0.14 nM 9.85
CHEMBL3086281 Ki = 0.15 nM 9.82
CHEMBL3085808 Ki = 0.16 nM 9.80
CHEMBL3085807 Ki = 0.18 nM 9.74
CHEMBL3085811 Ki = 0.24 nM 9.62
CHEMBL3087930 Ki = 0.25 nM 9.60
CHEMBL3086285 Ki = 0.28 nM 9.55
CHEMBL3085810 Ki = 0.3 nM 9.52
CHEMBL3085805 Ki = 0.52 nM 9.28