Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2416555

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

Binding
Binding affinity to orexin receptor 1 (unknown origin)
37
Total Activities
37
Compounds Tested
4
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin/Hypocretin receptor type 1 (CHEMBL5113)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective orexin receptor antagonists.
Lebold TP, Bonaventure P, Shireman BT.
Bioorg Med Chem Lett (2013) 23 : 4761 -4769
PubMed 23891187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.73 9.52
Kb 12 - -
IC50 6 7.94 8.30
Kd 2 5.84 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1272307 SB-649868 2.0 1 9.52
CHEMBL2413365 1 9.30
CHEMBL1083659 SUVOREXANT 4.0 1 9.22
CHEMBL2413366 1 9.00
CHEMBL2110363 1 8.96
CHEMBL2413521 1 8.96
CHEMBL2107822 FILOREXANT 2.0 1 8.60
CHEMBL2413523 1 8.30
CHEMBL2031493 1 8.22
CHEMBL2413367 1 8.22
CHEMBL2031484 1 8.10
CHEMBL522758 1 8.06
CHEMBL455136 ALMOREXANT 3.0 1 7.89
CHEMBL1334465 1 7.66
CHEMBL2111553 1 7.55
CHEMBL2413519 1 7.44
CHEMBL2031488 1 6.84
CHEMBL2413517 1 6.16
CHEMBL2385132 1 6.05
CHEMBL2385134 1 6.05
CHEMBL2385133 1 6.05
CHEMBL359632 1 5.78
CHEMBL2413518 1 5.51
CHEMBL2413520 1 5.36
CHEMBL2413527 1 -
CHEMBL2413526 1 -
CHEMBL2413525 1 -
CHEMBL2413524 1 -
CHEMBL2381071 1 -
CHEMBL2381072 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1272307 SB-649868 Ki = 0.3 nM 9.52
CHEMBL2413365 Ki = 0.5 nM 9.30
CHEMBL1083659 SUVOREXANT Ki = 0.6 nM 9.22
CHEMBL2413366 Ki = 1.0 nM 9.00
CHEMBL2110363 Ki = 1.1 nM 8.96
CHEMBL2413521 Ki = 1.1 nM 8.96
CHEMBL2107822 FILOREXANT Ki = 2.5 nM 8.60
CHEMBL2413523 IC50 = 5.0 nM 8.30
CHEMBL2031493 IC50 = 6.0 nM 8.22
CHEMBL2413367 IC50 = 6.0 nM 8.22
CHEMBL2031484 IC50 = 8.0 nM 8.10
CHEMBL522758 Ki = 8.7 nM 8.06
CHEMBL455136 ALMOREXANT Ki = 13.0 nM 7.89
CHEMBL1334465 Ki = 22.0 nM 7.66
CHEMBL2111553 Ki = 28.0 nM 7.55
CHEMBL2413519 Ki = 36.0 nM 7.44
CHEMBL2031488 IC50 = 145.0 nM 6.84
CHEMBL2413517 Kd = 696.0 nM 6.16
CHEMBL2385132 Ki = 900.0 nM 6.05
CHEMBL2385133 Ki = 900.0 nM 6.05
CHEMBL2385134 Ki = 900.0 nM 6.05
CHEMBL359632 Ki = 1644.0 nM 5.78
CHEMBL2413518 Kd = 3052.0 nM 5.51
CHEMBL2413520 Ki = 4363.0 nM 5.36
CHEMBL142009 IC50 > 10000.0 nM -
CHEMBL1771571 Kb = 64.2 nM -
CHEMBL2413522 Kb = 1.6 nM -
CHEMBL2413364 Kb = 1.0 nM -
CHEMBL2413363 Kb = 0.8 nM -
CHEMBL2413528 Kb = 0.5 nM -
CHEMBL2381098 Kb = 5.0 nM -
CHEMBL2381072 Kb = 158.0 nM -
CHEMBL2381071 Kb = 31.6 nM -
CHEMBL2413524 Kb = 0.6 nM -
CHEMBL2413525 Kb = 0.3 nM -
CHEMBL2413526 Kb = 0.3 nM -
CHEMBL2413527 Kb = 0.6 nM -