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Assay Detail

CHEMBL894442

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

Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanin-concentrating hormone receptor 1 (CHEMBL1075228)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR.
J Med Chem (2007) 50 : 3883 -3890
PubMed 17668922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.46 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185271 SNAP-7941 1 9.60
CHEMBL245231 1 8.74
CHEMBL242004 1 8.66
CHEMBL394569 1 8.30
CHEMBL245010 1 8.28
CHEMBL389129 1 8.09
CHEMBL389128 1 8.00
CHEMBL244791 1 7.75
CHEMBL244578 1 7.64
CHEMBL242003 1 7.57
CHEMBL244373 1 7.55
CHEMBL244374 1 7.51
CHEMBL245229 1 7.46
CHEMBL390212 1 7.37
CHEMBL244790 1 7.19
CHEMBL243794 1 7.16
CHEMBL244372 1 7.08
CHEMBL244004 1 7.00
CHEMBL245008 1 6.85
CHEMBL244163 1 6.70
CHEMBL395788 1 6.46
CHEMBL363548 CHLOROHALOPERIDOL 1 6.46
CHEMBL395789 1 6.44
CHEMBL244003 1 6.31
CHEMBL244576 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185271 SNAP-7941 Ki = 0.25 nM 9.60
CHEMBL245231 Ki = 1.8 nM 8.74
CHEMBL242004 Ki = 2.2 nM 8.66
CHEMBL394569 Ki = 5.0 nM 8.30
CHEMBL245010 Ki = 5.3 nM 8.28
CHEMBL389129 Ki = 8.2 nM 8.09
CHEMBL389128 Ki = 10.0 nM 8.00
CHEMBL244791 Ki = 18.0 nM 7.75
CHEMBL244578 Ki = 23.0 nM 7.64
CHEMBL242003 Ki = 27.0 nM 7.57
CHEMBL244373 Ki = 28.0 nM 7.55
CHEMBL244374 Ki = 31.0 nM 7.51
CHEMBL245229 Ki = 35.0 nM 7.46
CHEMBL390212 Ki = 43.0 nM 7.37
CHEMBL244790 Ki = 65.0 nM 7.19
CHEMBL243794 Ki = 70.0 nM 7.16
CHEMBL244372 Ki = 84.0 nM 7.08
CHEMBL244004 Ki = 100.0 nM 7.00
CHEMBL245008 Ki = 140.0 nM 6.85
CHEMBL244163 Ki = 200.0 nM 6.70
CHEMBL395788 Ki = 350.0 nM 6.46
CHEMBL363548 CHLOROHALOPERIDOL Ki = 350.0 nM 6.46
CHEMBL395789 Ki = 360.0 nM 6.44
CHEMBL244003 Ki = 490.0 nM 6.31
CHEMBL244576 Ki = 540.0 nM 6.27