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Assay Detail

CHEMBL4410510

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

Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanin-concentrating hormone receptor 1 (CHEMBL344)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a new small molecule chemotype of Melanin Concentrating Hormone Receptor-1 antagonists using pharmacophore-based virtual screening.
Helal MA, Chittiboyina AG, Avery MA.
Bioorg Med Chem Lett (2019) 29 : 126741 -126741
PubMed 31678007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 7.01 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176219 1 9.77
CHEMBL176159 1 9.51
CHEMBL178997 1 9.39
CHEMBL175993 1 9.06
CHEMBL361215 1 9.01
CHEMBL367532 1 8.92
CHEMBL179437 1 8.92
CHEMBL215030 1 8.66
CHEMBL179353 1 8.66
CHEMBL176548 1 8.59
CHEMBL367156 1 8.51
CHEMBL209109 1 8.46
CHEMBL377843 1 8.32
CHEMBL4465399 1 8.31
CHEMBL190780 1 8.28
CHEMBL2112988 1 8.27
CHEMBL360731 1 8.26
CHEMBL4444299 1 8.17
CHEMBL182150 1 8.08
CHEMBL429895 1 7.99
CHEMBL377864 1 7.70
CHEMBL215964 1 7.68
CHEMBL214432 1 7.62
CHEMBL176024 1 7.62
CHEMBL175860 1 7.41
CHEMBL4476156 1 7.40
CHEMBL208635 1 7.36
CHEMBL179325 1 7.30
CHEMBL386039 1 7.15
CHEMBL217605 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176219 IC50 = 0.17 nM 9.77
CHEMBL176159 IC50 = 0.31 nM 9.51
CHEMBL178997 IC50 = 0.41 nM 9.39
CHEMBL175993 IC50 = 0.88 nM 9.06
CHEMBL361215 IC50 = 0.98 nM 9.01
CHEMBL367532 IC50 = 1.2 nM 8.92
CHEMBL179437 IC50 = 1.2 nM 8.92
CHEMBL215030 IC50 = 2.2 nM 8.66
CHEMBL179353 IC50 = 2.2 nM 8.66
CHEMBL176548 IC50 = 2.6 nM 8.59
CHEMBL367156 IC50 = 3.1 nM 8.51
CHEMBL209109 IC50 = 3.5 nM 8.46
CHEMBL377843 IC50 = 4.8 nM 8.32
CHEMBL4465399 IC50 = 4.9 nM 8.31
CHEMBL190780 IC50 = 5.2 nM 8.28
CHEMBL2112988 IC50 = 5.4 nM 8.27
CHEMBL360731 IC50 = 5.5 nM 8.26
CHEMBL4444299 IC50 = 6.8 nM 8.17
CHEMBL182150 IC50 = 8.28 nM 8.08
CHEMBL429895 IC50 = 10.3 nM 7.99
CHEMBL377864 IC50 = 20.0 nM 7.70
CHEMBL215964 IC50 = 21.0 nM 7.68
CHEMBL214432 IC50 = 24.0 nM 7.62
CHEMBL176024 IC50 = 24.0 nM 7.62
CHEMBL175860 IC50 = 39.0 nM 7.41
CHEMBL4476156 IC50 = 40.0 nM 7.40
CHEMBL208635 IC50 = 44.0 nM 7.36
CHEMBL179325 IC50 = 50.0 nM 7.30
CHEMBL386039 IC50 = 71.0 nM 7.15
CHEMBL217605 IC50 = 82.0 nM 7.09
CHEMBL379802 IC50 = 95.0 nM 7.02
CHEMBL550545 IC50 = 100.0 nM 7.00
CHEMBL4461504 IC50 = 105.0 nM 6.98
CHEMBL4460423 IC50 = 129.0 nM 6.89
CHEMBL212254 IC50 = 130.0 nM 6.89
CHEMBL378261 IC50 = 132.0 nM 6.88
CHEMBL267320 IC50 = 140.0 nM 6.85
CHEMBL424895 IC50 = 150.0 nM 6.82
CHEMBL217196 IC50 = 150.0 nM 6.82
CHEMBL4571110 IC50 = 228.0 nM 6.64
CHEMBL562016 IC50 = 270.0 nM 6.57
CHEMBL179872 IC50 = 280.0 nM 6.55
CHEMBL370222 IC50 = 280.0 nM 6.55
CHEMBL175874 IC50 = 300.0 nM 6.52
CHEMBL213771 IC50 = 300.0 nM 6.52
CHEMBL214858 IC50 = 320.0 nM 6.50
CHEMBL268385 IC50 = 405.0 nM 6.39
CHEMBL425445 IC50 = 497.0 nM 6.30
CHEMBL217860 IC50 = 750.0 nM 6.12
CHEMBL4524539 IC50 = 890.0 nM 6.05