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Assay Detail

CHEMBL840206

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

Binding
Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melatonin receptor type 1B (CHEMBL1946)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.
Lucini V, Pannacci M, Scaglione F, Fraschini F, Rivara S, Mor M, Bordi F, Plazzi PV, Spadoni G, Bedini A, Piersanti G, Diamantini G, Tarzia G.
J Med Chem (2004) 47 : 4202 -4212
PubMed 15293992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.86 9.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189414 1 9.79
CHEMBL189395 1 9.61
CHEMBL45 MELATONIN 4.0 1 9.55
CHEMBL189449 1 9.18
CHEMBL427516 1 9.05
CHEMBL363321 1 7.52
CHEMBL364806 1 7.42
CHEMBL187160 1 7.40
CHEMBL365249 1 7.07
CHEMBL364835 1 7.05
CHEMBL362133 1 6.90
CHEMBL360600 1 6.70
CHEMBL364845 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189414 Ki = 0.1622 nM 9.79
CHEMBL189395 Ki = 0.2455 nM 9.61
CHEMBL45 MELATONIN Ki = 0.2818 nM 9.55
CHEMBL189449 Ki = 0.6607 nM 9.18
CHEMBL427516 Ki = 0.8913 nM 9.05
CHEMBL363321 Ki = 30.2 nM 7.52
CHEMBL364806 Ki = 38.02 nM 7.42
CHEMBL187160 Ki = 39.81 nM 7.40
CHEMBL365249 Ki = 85.11 nM 7.07
CHEMBL364835 Ki = 89.13 nM 7.05
CHEMBL362133 Ki = 125.89 nM 6.90
CHEMBL360600 Ki = 199.53 nM 6.70
CHEMBL364845 Ki = 10964.78 nM 4.96