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Assay Detail

CHEMBL1007895

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Binding
Binding affinity to OX1 receptor
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
Boss C, Brisbare-Roch C, Jenck F.
J Med Chem (2009) 52 : 891 -903
PubMed 19199652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.92 8.30
Kd 3 8.07 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522758 1 8.35
CHEMBL359632 1 8.30
CHEMBL2110363 1 8.29
CHEMBL185088 1 8.20
CHEMBL185136 1 7.70
CHEMBL1334465 1 7.57
CHEMBL185093 1 7.40
CHEMBL361716 1 7.20
CHEMBL182473 1 7.20
CHEMBL185382 1 7.10
CHEMBL185435 1 7.10
CHEMBL363951 1 7.00
CHEMBL363743 1 7.00
CHEMBL183576 1 6.90
CHEMBL184936 1 6.60
CHEMBL361748 1 6.40
CHEMBL360377 1 6.30
CHEMBL185080 1 6.00
CHEMBL184384 1 5.60
CHEMBL183786 1 5.60
CHEMBL185219 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522758 Kd = 4.467 nM 8.35
CHEMBL359632 Ki = 5.012 nM 8.30
CHEMBL2110363 Kd = 5.129 nM 8.29
CHEMBL185088 Ki = 6.31 nM 8.20
CHEMBL185136 Ki = 19.95 nM 7.70
CHEMBL1334465 Kd = 26.92 nM 7.57
CHEMBL185093 Ki = 39.81 nM 7.40
CHEMBL361716 Ki = 63.1 nM 7.20
CHEMBL182473 Ki = 63.1 nM 7.20
CHEMBL185382 Ki = 79.43 nM 7.10
CHEMBL185435 Ki = 79.43 nM 7.10
CHEMBL363951 Ki = 100.0 nM 7.00
CHEMBL363743 Ki = 100.0 nM 7.00
CHEMBL183576 Ki = 125.89 nM 6.90
CHEMBL184936 Ki = 251.19 nM 6.60
CHEMBL361748 Ki = 398.11 nM 6.40
CHEMBL360377 Ki = 501.19 nM 6.30
CHEMBL185080 Ki = 1000.0 nM 6.00
CHEMBL184384 Ki = 2511.89 nM 5.60
CHEMBL183786 Ki = 2511.89 nM 5.60
CHEMBL185219 Ki > 5011.87 nM -