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Assay Detail

CHEMBL908288

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

Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cells
46
Total Activities
46
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

Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Lynch JK, Freeman JC, Judd AS, Iyengar R, Mulhern M, Zhao G, Napier JJ, Wodka D, Brodjian S, Dayton BD, Falls D, Ogiela C, Reilly RM, Campbell TJ, Polakowski JS, Hernandez L, Marsh KC, Shapiro R, Knourek-Segel V, Droz B, Bush E, Brune M, Preusser LC, Fryer RM, Reinhart GA, Houseman K, Diaz G, Mikhail A, Limberis JT, Sham HL, Collins CA, Kym PR.
J Med Chem (2006) 49 : 6569 -6584
PubMed 17064075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 7.29 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277531 1 8.70
CHEMBL217442 1 8.70
CHEMBL387178 1 8.70
CHEMBL204828 1 8.52
CHEMBL387418 1 8.52
CHEMBL214021 1 8.52
CHEMBL217789 1 8.30
CHEMBL206081 1 7.96
CHEMBL216225 1 7.92
CHEMBL217593 1 7.89
CHEMBL217105 1 7.66
CHEMBL214768 1 7.62
CHEMBL386021 1 7.62
CHEMBL217400 1 7.51
CHEMBL217706 1 7.50
CHEMBL384487 1 7.41
CHEMBL387417 1 7.33
CHEMBL387309 1 7.28
CHEMBL217707 1 7.24
CHEMBL214377 1 7.23
CHEMBL213761 1 7.22
CHEMBL214731 1 7.19
CHEMBL213715 1 7.19
CHEMBL214767 1 7.18
CHEMBL425448 1 7.14
CHEMBL2113245 1 7.12
CHEMBL214413 1 7.04
CHEMBL441542 1 7.00
CHEMBL387219 1 6.88
CHEMBL214278 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277531 IC50 = 2.0 nM 8.70
CHEMBL387178 IC50 = 2.0 nM 8.70
CHEMBL217442 IC50 = 2.0 nM 8.70
CHEMBL204828 IC50 = 3.0 nM 8.52
CHEMBL387418 IC50 = 3.0 nM 8.52
CHEMBL214021 IC50 = 3.0 nM 8.52
CHEMBL217789 IC50 = 5.0 nM 8.30
CHEMBL206081 IC50 = 11.0 nM 7.96
CHEMBL216225 IC50 = 12.0 nM 7.92
CHEMBL217593 IC50 = 13.0 nM 7.89
CHEMBL217105 IC50 = 22.0 nM 7.66
CHEMBL214768 IC50 = 24.0 nM 7.62
CHEMBL386021 IC50 = 24.0 nM 7.62
CHEMBL217400 IC50 = 31.0 nM 7.51
CHEMBL217706 IC50 = 32.0 nM 7.50
CHEMBL384487 IC50 = 39.0 nM 7.41
CHEMBL387417 IC50 = 47.0 nM 7.33
CHEMBL387309 IC50 = 53.0 nM 7.28
CHEMBL217707 IC50 = 57.0 nM 7.24
CHEMBL214377 IC50 = 59.0 nM 7.23
CHEMBL213761 IC50 = 60.0 nM 7.22
CHEMBL214731 IC50 = 65.0 nM 7.19
CHEMBL213715 IC50 = 64.0 nM 7.19
CHEMBL214767 IC50 = 66.0 nM 7.18
CHEMBL425448 IC50 = 73.0 nM 7.14
CHEMBL2113245 IC50 = 75.0 nM 7.12
CHEMBL214413 IC50 = 91.0 nM 7.04
CHEMBL441542 IC50 = 99.0 nM 7.00
CHEMBL387219 IC50 = 132.0 nM 6.88
CHEMBL214278 IC50 = 159.0 nM 6.80
CHEMBL402868 IC50 = 178.0 nM 6.75
CHEMBL217925 IC50 = 187.0 nM 6.73
CHEMBL216577 IC50 = 351.0 nM 6.46
CHEMBL213658 IC50 = 393.0 nM 6.41
CHEMBL214075 IC50 = 427.0 nM 6.37
CHEMBL216777 IC50 = 566.0 nM 6.25
CHEMBL216133 IC50 = 734.0 nM 6.13
CHEMBL384458 IC50 = 1140.0 nM 5.94
CHEMBL215631 IC50 = 1480.0 nM 5.83
CHEMBL216680 IC50 = 1690.0 nM 5.77
CHEMBL216456 IC50 > 2000.0 nM -
CHEMBL214766 IC50 > 2000.0 nM -
CHEMBL425435 IC50 > 2000.0 nM -
CHEMBL217857 IC50 > 2000.0 nM -
CHEMBL216190 IC50 > 2000.0 nM -
CHEMBL214679 IC50 > 700.0 nM -