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Assay Detail

CHEMBL713108

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

Binding
Binding affinity against Melatonin receptor 3 (MT3) of Syrian hamster brain and peripheral organs
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
Uchikawa O, Fukatsu K, Tokunoh R, Kawada M, Matsumoto K, Imai Y, Hinuma S, Kato K, Nishikawa H, Hirai K, Miyamoto M, Ohkawa S.
J Med Chem (2002) 45 : 4222 -4239
PubMed 12213063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.95 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 7.56
CHEMBL132405 1 7.28
CHEMBL337838 1 6.62
CHEMBL335427 1 6.59
CHEMBL134435 1 6.31
CHEMBL135072 1 5.97
CHEMBL134330 1 5.90
CHEMBL133775 (R)-RAMELTEON 1 5.64
CHEMBL336507 1 5.59
CHEMBL1218 RAMELTEON 4.0 1 5.58
CHEMBL135108 1 5.32
CHEMBL336536 1 5.27
CHEMBL336960 1 5.23
CHEMBL134102 1 5.22
CHEMBL334851 1 5.21
CHEMBL334736 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN Ki = 27.6 nM 7.56
CHEMBL132405 Ki = 52.8 nM 7.28
CHEMBL337838 Ki = 237.0 nM 6.62
CHEMBL335427 Ki = 255.0 nM 6.59
CHEMBL134435 Ki = 492.0 nM 6.31
CHEMBL135072 Ki = 1070.0 nM 5.97
CHEMBL134330 Ki = 1250.0 nM 5.90
CHEMBL133775 (R)-RAMELTEON Ki = 2270.0 nM 5.64
CHEMBL336507 Ki = 2560.0 nM 5.59
CHEMBL1218 RAMELTEON Ki = 2600.0 nM 5.58
CHEMBL135108 Ki = 4790.0 nM 5.32
CHEMBL336536 Ki = 5390.0 nM 5.27
CHEMBL336960 Ki = 5830.0 nM 5.23
CHEMBL134102 Ki = 5960.0 nM 5.22
CHEMBL334851 Ki = 6220.0 nM 5.21
CHEMBL334736 Ki > 10000.0 nM -