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Assay Detail

CHEMBL5733331

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

Binding
Cell-based Functional Assay: Measurement of [Ca2+]i using a FLIPR: CHO-OX1 or CHO-OX2 cells are seeded into black-walled clear-base 384-well plates (Costar) at a density of 20,000 cells per well in F12-K medium supplemented with 10% FBS and selection antibiotic (500 ug/ml G418 or 15 ug/ml Blasticidin) and cultured overnight. The cells are incubated with equal volume of calcium4 loading buffer (Molecular Devices, Inc.) containing 2.5 mM probenecid at 37° C. for 30 min, followed by putative OX1 or OX2 receptor antagonists (dose-range 0.1 nM-10 μM) for another 30 min.
ChEMBL ↗
981
Total Activities
315
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin receptor type 2 (CHEMBL4792) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted prolines/piperidines as orexin receptor antagonists
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 327 6.32 8.70
kon 327 - -
k_off 327 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5994245 — — 3 8.70
CHEMBL6057686 — — 3 8.52
CHEMBL5753451 — — 3 8.40
CHEMBL6029935 — — 3 8.30
CHEMBL5840325 — — 3 8.15
CHEMBL6041150 — — 3 8.10
CHEMBL5933560 — — 3 8.10
CHEMBL2031485 — — 3 8.10
CHEMBL5953846 — — 3 8.10
CHEMBL5854442 — — 3 8.00
CHEMBL6057653 — — 3 7.85
CHEMBL2031490 — — 3 7.77
CHEMBL6058561 — — 3 7.60
CHEMBL6061615 — — 3 7.60
CHEMBL5742009 — — 3 7.52
CHEMBL5976505 — — 3 7.44
CHEMBL5960586 — — 3 7.42
CHEMBL6015540 — — 3 7.40
CHEMBL6043379 — — 3 7.40
CHEMBL2031487 — — 3 7.40
CHEMBL5771582 — — 3 7.35
CHEMBL6028684 — — 3 7.32
CHEMBL2031491 — — 3 7.22
CHEMBL5845554 — — 3 7.16
CHEMBL5967554 — — 3 7.16
CHEMBL5785648 — — 3 7.12
CHEMBL5985902 — — 3 7.12
CHEMBL2031489 — — 3 7.07
CHEMBL5898351 — — 3 7.07
CHEMBL5893020 — — 3 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5994245 — IC50 = 2.0 nM 8.70
CHEMBL6057686 — IC50 = 3.0 nM 8.52
CHEMBL5753451 — IC50 = 4.0 nM 8.40
CHEMBL6029935 — IC50 = 5.0 nM 8.30
CHEMBL5840325 — IC50 = 7.0 nM 8.15
CHEMBL5933560 — IC50 = 8.0 nM 8.10
CHEMBL6041150 — IC50 = 8.0 nM 8.10
CHEMBL2031485 — IC50 = 8.0 nM 8.10
CHEMBL5953846 — IC50 = 8.0 nM 8.10
CHEMBL5854442 — IC50 = 10.0 nM 8.00
CHEMBL6057653 — IC50 = 14.0 nM 7.85
CHEMBL2031490 — IC50 = 17.0 nM 7.77
CHEMBL6058561 — IC50 = 25.0 nM 7.60
CHEMBL6061615 — IC50 = 25.0 nM 7.60
CHEMBL5742009 — IC50 = 30.0 nM 7.52
CHEMBL5976505 — IC50 = 36.0 nM 7.44
CHEMBL5960586 — IC50 = 38.0 nM 7.42
CHEMBL2031487 — IC50 = 40.0 nM 7.40
CHEMBL6043379 — IC50 = 40.0 nM 7.40
CHEMBL6015540 — IC50 = 40.0 nM 7.40
CHEMBL5771582 — IC50 = 45.0 nM 7.35
CHEMBL6028684 — IC50 = 48.0 nM 7.32
CHEMBL2031491 — IC50 = 60.0 nM 7.22
CHEMBL5967554 — IC50 = 70.0 nM 7.16
CHEMBL5845554 — IC50 = 70.0 nM 7.16
CHEMBL5985902 — IC50 = 75.0 nM 7.12
CHEMBL5785648 — IC50 = 75.0 nM 7.12
CHEMBL5898351 — IC50 = 86.0 nM 7.07
CHEMBL2031489 — IC50 = 85.0 nM 7.07
CHEMBL5893020 — IC50 = 91.0 nM 7.04
CHEMBL2031484 — IC50 = 95.0 nM 7.02
CHEMBL2031492 — IC50 = 100.0 nM 7.00
CHEMBL5740980 — IC50 = 100.0 nM 7.00
CHEMBL5860928 — IC50 = 130.0 nM 6.89
CHEMBL6060054 — IC50 = 130.0 nM 6.89
CHEMBL5903849 — IC50 = 140.0 nM 6.85
CHEMBL5977537 — IC50 = 140.0 nM 6.85
CHEMBL6033386 — IC50 = 140.0 nM 6.85
CHEMBL5744146 — IC50 = 160.0 nM 6.80
CHEMBL5947194 — IC50 = 160.0 nM 6.80
CHEMBL5912391 — IC50 = 190.0 nM 6.72
CHEMBL5955231 — IC50 = 220.0 nM 6.66
CHEMBL5956386 — IC50 = 230.0 nM 6.64
CHEMBL2031486 — IC50 = 237.0 nM 6.62
CHEMBL5800593 — IC50 = 250.0 nM 6.60
CHEMBL5789395 — IC50 = 253.0 nM 6.60
CHEMBL6003372 — IC50 = 260.0 nM 6.58
CHEMBL5898556 — IC50 = 320.0 nM 6.50
CHEMBL5971415 — IC50 = 340.0 nM 6.47
CHEMBL5873036 — IC50 = 350.0 nM 6.46