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Assay Detail

CHEMBL908289

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Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 6.54 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387178 — — 1 7.89
CHEMBL217442 — — 1 7.80
CHEMBL214021 — — 1 7.54
CHEMBL277531 — — 1 7.17
CHEMBL387418 — — 1 7.15
CHEMBL206081 — — 1 7.14
CHEMBL217789 — — 1 7.10
CHEMBL217706 — — 1 7.09
CHEMBL204828 — — 1 7.08
CHEMBL217593 — — 1 7.00
CHEMBL387417 — — 1 6.86
CHEMBL213715 — — 1 6.80
CHEMBL214768 — — 1 6.78
CHEMBL425448 — — 1 6.77
CHEMBL214767 — — 1 6.72
CHEMBL214731 — — 1 6.71
CHEMBL217105 — — 1 6.58
CHEMBL217400 — — 1 6.41
CHEMBL387309 — — 1 6.39
CHEMBL214413 — — 1 6.38
CHEMBL214377 — — 1 6.28
CHEMBL384487 — — 1 6.24
CHEMBL213761 — — 1 6.23
CHEMBL217707 — — 1 6.22
CHEMBL214278 — — 1 6.10
CHEMBL216225 — — 1 6.01
CHEMBL216133 — — 1 5.69
CHEMBL216777 — — 1 5.67
CHEMBL441542 — — 1 5.57
CHEMBL402868 — — 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387178 — IC50 = 13.0 nM 7.89
CHEMBL217442 — IC50 = 16.0 nM 7.80
CHEMBL214021 — IC50 = 29.0 nM 7.54
CHEMBL277531 — IC50 = 67.0 nM 7.17
CHEMBL387418 — IC50 = 71.0 nM 7.15
CHEMBL206081 — IC50 = 73.0 nM 7.14
CHEMBL217789 — IC50 = 79.0 nM 7.10
CHEMBL217706 — IC50 = 82.0 nM 7.09
CHEMBL204828 — IC50 = 83.0 nM 7.08
CHEMBL217593 — IC50 = 101.0 nM 7.00
CHEMBL387417 — IC50 = 137.0 nM 6.86
CHEMBL213715 — IC50 = 160.0 nM 6.80
CHEMBL214768 — IC50 = 168.0 nM 6.78
CHEMBL425448 — IC50 = 171.0 nM 6.77
CHEMBL214767 — IC50 = 192.0 nM 6.72
CHEMBL214731 — IC50 = 196.0 nM 6.71
CHEMBL217105 — IC50 = 266.0 nM 6.58
CHEMBL217400 — IC50 = 390.0 nM 6.41
CHEMBL387309 — IC50 = 411.0 nM 6.39
CHEMBL214413 — IC50 = 418.0 nM 6.38
CHEMBL214377 — IC50 = 529.0 nM 6.28
CHEMBL384487 — IC50 = 581.0 nM 6.24
CHEMBL213761 — IC50 = 592.0 nM 6.23
CHEMBL217707 — IC50 = 601.0 nM 6.22
CHEMBL214278 — IC50 = 789.0 nM 6.10
CHEMBL216225 — IC50 = 966.0 nM 6.01
CHEMBL216133 — IC50 = 2050.0 nM 5.69
CHEMBL216777 — IC50 = 2150.0 nM 5.67
CHEMBL441542 — IC50 = 2720.0 nM 5.57
CHEMBL402868 — IC50 = 3070.0 nM 5.51
CHEMBL2113245 — IC50 = 4750.0 nM 5.32
CHEMBL384458 — IC50 = 8300.0 nM 5.08
CHEMBL216190 — IC50 - — -
CHEMBL217857 — IC50 - — -
CHEMBL425435 — IC50 - — -
CHEMBL214766 — IC50 - — -
CHEMBL216456 — IC50 - — -
CHEMBL215631 — IC50 > 10000.0 nM -
CHEMBL386021 — IC50 > 10000.0 nM -
CHEMBL387219 — IC50 > 9000.0 nM -
CHEMBL217925 — IC50 > 6000.0 nM -
CHEMBL216577 — IC50 - — -
CHEMBL213658 — IC50 - — -
CHEMBL216680 — IC50 > 10000.0 nM -
CHEMBL214075 — IC50 - — -
CHEMBL214679 — IC50 - — -