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Assay Detail

CHEMBL832324

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

Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
Vasudevan A, Wodka D, Verzal MK, Souers AJ, Gao J, Brodjian S, Fry D, Dayton B, Marsh KC, Hernandez LE, Ogiela CA, Collins CA, Kym PR.
Bioorg Med Chem Lett (2004) 14 : 4879 -4882
PubMed 15341943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.77 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182261 1 9.40
CHEMBL184417 1 9.05
CHEMBL359995 1 9.00
CHEMBL362768 1 9.00
CHEMBL183032 1 9.00
CHEMBL184243 1 8.70
CHEMBL182575 1 8.70
CHEMBL184581 1 8.52
CHEMBL185271 SNAP-7941 1 8.52
CHEMBL184080 1 8.30
CHEMBL363464 1 8.30
CHEMBL363664 1 8.30
CHEMBL364210 1 8.22
CHEMBL184191 1 8.15
CHEMBL187162 1 8.00
CHEMBL361878 1 8.00
CHEMBL187847 1 8.00
CHEMBL360393 1 8.00
CHEMBL363683 1 8.00
CHEMBL183159 2 7.70
CHEMBL184590 1 7.52
CHEMBL188058 1 7.52
CHEMBL184477 1 7.40
CHEMBL184589 1 7.30
CHEMBL362150 1 7.30
CHEMBL361262 1 7.22
CHEMBL187003 1 7.16
CHEMBL185236 1 7.10
CHEMBL365041 1 7.10
CHEMBL178707 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182261 IC50 = 0.4 nM 9.40
CHEMBL184417 IC50 = 0.9 nM 9.05
CHEMBL362768 IC50 = 1.0 nM 9.00
CHEMBL183032 IC50 = 1.0 nM 9.00
CHEMBL359995 IC50 = 1.0 nM 9.00
CHEMBL184243 IC50 = 2.0 nM 8.70
CHEMBL182575 IC50 = 2.0 nM 8.70
CHEMBL185271 SNAP-7941 IC50 = 3.0 nM 8.52
CHEMBL184581 IC50 = 3.0 nM 8.52
CHEMBL363664 IC50 = 5.0 nM 8.30
CHEMBL363464 IC50 = 5.0 nM 8.30
CHEMBL184080 IC50 = 5.0 nM 8.30
CHEMBL364210 IC50 = 6.0 nM 8.22
CHEMBL184191 IC50 = 7.0 nM 8.15
CHEMBL363683 IC50 = 10.0 nM 8.00
CHEMBL187162 IC50 = 10.0 nM 8.00
CHEMBL360393 IC50 = 10.0 nM 8.00
CHEMBL187847 IC50 = 10.0 nM 8.00
CHEMBL361878 IC50 = 10.0 nM 8.00
CHEMBL183159 IC50 = 20.0 nM 7.70
CHEMBL184590 IC50 = 30.0 nM 7.52
CHEMBL188058 IC50 = 30.0 nM 7.52
CHEMBL184477 IC50 = 40.0 nM 7.40
CHEMBL362150 IC50 = 50.0 nM 7.30
CHEMBL183159 IC50 = 50.0 nM 7.30
CHEMBL184589 IC50 = 50.0 nM 7.30
CHEMBL361262 IC50 = 60.0 nM 7.22
CHEMBL187003 IC50 = 70.0 nM 7.16
CHEMBL365041 IC50 = 80.0 nM 7.10
CHEMBL185236 IC50 = 80.0 nM 7.10
CHEMBL178707 IC50 = 85.0 nM 7.07
CHEMBL364377 IC50 = 90.0 nM 7.05
CHEMBL184087 IC50 = 100.0 nM 7.00
CHEMBL369116 IC50 = 100.0 nM 7.00
CHEMBL364399 IC50 = 210.0 nM 6.68
CHEMBL362309 IC50 = 520.0 nM 6.28
CHEMBL363701 IC50 = 530.0 nM 6.28
CHEMBL363220 IC50 = 660.0 nM 6.18