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Assay Detail

CHEMBL860146

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

Binding
Binding affinity to human MCHr1 from neuronal IMR32 cells
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

Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Vasudevan A, Souers AJ, Freeman JC, Verzal MK, Gao J, Mulhern MM, Wodka D, Lynch JK, Engstrom KM, Wagaw SH, Brodjian S, Dayton B, Falls DH, Bush E, Brune M, Shapiro RD, Marsh KC, Hernandez LE, Collins CA, Kym PR.
Bioorg Med Chem Lett (2005) 15 : 5293 -5297
PubMed 16203136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.32 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427367 1 8.30
CHEMBL196973 1 8.22
CHEMBL199025 1 8.15
CHEMBL371222 1 8.10
CHEMBL197232 1 8.05
CHEMBL198835 1 7.70
CHEMBL383359 1 7.70
CHEMBL197497 1 7.70
CHEMBL265540 1 7.70
CHEMBL369986 1 7.70
CHEMBL372848 1 7.70
CHEMBL199222 1 7.52
CHEMBL381013 1 7.52
CHEMBL380782 1 7.40
CHEMBL198890 1 7.40
CHEMBL370576 1 7.40
CHEMBL370361 1 7.30
CHEMBL198789 1 7.30
CHEMBL197395 1 7.30
CHEMBL198588 1 7.16
CHEMBL197283 1 7.00
CHEMBL196972 1 6.96
CHEMBL197281 1 6.82
CHEMBL370360 1 6.70
CHEMBL197059 1 6.66
CHEMBL197058 1 6.62
CHEMBL370222 1 6.55
CHEMBL198692 1 6.48
CHEMBL197023 1 6.36
CHEMBL197485 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427367 IC50 = 5.0 nM 8.30
CHEMBL196973 IC50 = 6.0 nM 8.22
CHEMBL199025 IC50 = 7.0 nM 8.15
CHEMBL371222 IC50 = 8.0 nM 8.10
CHEMBL197232 IC50 = 9.0 nM 8.05
CHEMBL198835 IC50 = 20.0 nM 7.70
CHEMBL383359 IC50 = 20.0 nM 7.70
CHEMBL197497 IC50 = 20.0 nM 7.70
CHEMBL265540 IC50 = 20.0 nM 7.70
CHEMBL369986 IC50 = 20.0 nM 7.70
CHEMBL372848 IC50 = 20.0 nM 7.70
CHEMBL199222 IC50 = 30.0 nM 7.52
CHEMBL381013 IC50 = 30.0 nM 7.52
CHEMBL380782 IC50 = 40.0 nM 7.40
CHEMBL370576 IC50 = 40.0 nM 7.40
CHEMBL198890 IC50 = 40.0 nM 7.40
CHEMBL370361 IC50 = 50.0 nM 7.30
CHEMBL198789 IC50 = 50.0 nM 7.30
CHEMBL197395 IC50 = 50.0 nM 7.30
CHEMBL198588 IC50 = 70.0 nM 7.16
CHEMBL197283 IC50 = 100.0 nM 7.00
CHEMBL196972 IC50 = 110.0 nM 6.96
CHEMBL197281 IC50 = 150.0 nM 6.82
CHEMBL370360 IC50 = 200.0 nM 6.70
CHEMBL197059 IC50 = 220.0 nM 6.66
CHEMBL197058 IC50 = 240.0 nM 6.62
CHEMBL370222 IC50 = 280.0 nM 6.55
CHEMBL198692 IC50 = 330.0 nM 6.48
CHEMBL197023 IC50 = 440.0 nM 6.36
CHEMBL197485 IC50 = 850.0 nM 6.07
CHEMBL383150 IC50 > 2000.0 nM -