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Assay Detail

CHEMBL855227

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

Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Vasudevan A, LaMarche MJ, Blackburn C, Che JL, Luchaco-Cullis CA, Lai S, Marsilje TH, Patane MA, Souers AJ, Wodka D, Geddes B, Chen S, Brodjian S, Falls DH, Dayton BD, Bush E, Brune M, Shapiro RD, Marsh KC, Hernandez LE, Sham HL, Collins CA, Kym PR.
Bioorg Med Chem Lett (2005) 15 : 4174 -4179
PubMed 16085414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.12 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196277 1 8.10
CHEMBL196681 1 8.05
CHEMBL194697 1 7.80
CHEMBL194731 1 7.70
CHEMBL194583 1 7.70
CHEMBL371700 1 7.70
CHEMBL193576 1 7.70
CHEMBL195511 1 7.52
CHEMBL194759 1 7.52
CHEMBL365788 1 7.52
CHEMBL434934 1 7.52
CHEMBL194726 1 7.40
CHEMBL371129 1 7.40
CHEMBL364522 1 7.30
CHEMBL363169 1 7.30
CHEMBL196223 1 7.22
CHEMBL373266 1 7.16
CHEMBL274254 1 7.16
CHEMBL365360 1 7.16
CHEMBL195255 1 7.05
CHEMBL373235 1 7.00
CHEMBL365734 1 7.00
CHEMBL196898 1 6.70
CHEMBL194342 1 6.66
CHEMBL194531 1 6.62
CHEMBL196620 1 6.43
CHEMBL427542 1 6.43
CHEMBL196591 1 6.29
CHEMBL195435 1 5.97
CHEMBL193489 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196277 IC50 = 8.0 nM 8.10
CHEMBL196681 IC50 = 9.0 nM 8.05
CHEMBL194697 IC50 = 16.0 nM 7.80
CHEMBL194731 IC50 = 20.0 nM 7.70
CHEMBL194583 IC50 = 20.0 nM 7.70
CHEMBL371700 IC50 = 20.0 nM 7.70
CHEMBL193576 IC50 = 20.0 nM 7.70
CHEMBL195511 IC50 = 30.0 nM 7.52
CHEMBL194759 IC50 = 30.0 nM 7.52
CHEMBL365788 IC50 = 30.0 nM 7.52
CHEMBL434934 IC50 = 30.0 nM 7.52
CHEMBL194726 IC50 = 40.0 nM 7.40
CHEMBL371129 IC50 = 40.0 nM 7.40
CHEMBL364522 IC50 = 50.0 nM 7.30
CHEMBL363169 IC50 = 50.0 nM 7.30
CHEMBL196223 IC50 = 60.0 nM 7.22
CHEMBL373266 IC50 = 70.0 nM 7.16
CHEMBL274254 IC50 = 70.0 nM 7.16
CHEMBL365360 IC50 = 70.0 nM 7.16
CHEMBL195255 IC50 = 90.0 nM 7.05
CHEMBL373235 IC50 = 100.0 nM 7.00
CHEMBL365734 IC50 = 100.0 nM 7.00
CHEMBL196898 IC50 = 200.0 nM 6.70
CHEMBL194342 IC50 = 220.0 nM 6.66
CHEMBL194531 IC50 = 240.0 nM 6.62
CHEMBL196620 IC50 = 370.0 nM 6.43
CHEMBL427542 IC50 = 370.0 nM 6.43
CHEMBL196591 IC50 = 510.0 nM 6.29
CHEMBL195435 IC50 = 1060.0 nM 5.97
CHEMBL193489 IC50 = 1220.0 nM 5.91
CHEMBL196168 IC50 = 1940.0 nM 5.71