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Assay Detail

CHEMBL3887404

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

Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL3737)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Morpholino compounds, uses and methods
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 5.96 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3946661 1 9.22
CHEMBL3986651 1 6.76
CHEMBL3900699 1 6.43
CHEMBL4112056 1 6.42
CHEMBL4110261 1 6.27
CHEMBL3946540 1 6.26
CHEMBL3941579 1 6.23
CHEMBL3897835 1 6.19
CHEMBL3915107 1 5.86
CHEMBL4109801 1 5.83
CHEMBL4115493 1 5.73
CHEMBL4112007 1 5.64
CHEMBL4108986 1 5.54
CHEMBL4112610 1 5.30
CHEMBL4112412 1 5.20
CHEMBL4115017 1 5.18
CHEMBL4107302 1 5.13
CHEMBL4109218 1 5.12
CHEMBL3936595 1 5.00
CHEMBL4114519 1 -
CHEMBL4112009 1 -
CHEMBL4110219 1 -
CHEMBL4115505 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3946661 Ki = 0.6 nM 9.22
CHEMBL3986651 Ki = 174.0 nM 6.76
CHEMBL3900699 Ki = 371.0 nM 6.43
CHEMBL4112056 Ki = 384.0 nM 6.42
CHEMBL4110261 Ki = 540.0 nM 6.27
CHEMBL3946540 Ki = 545.0 nM 6.26
CHEMBL3941579 Ki = 592.0 nM 6.23
CHEMBL3897835 Ki = 644.0 nM 6.19
CHEMBL3915107 Ki = 1388.0 nM 5.86
CHEMBL4109801 Ki = 1469.0 nM 5.83
CHEMBL4115493 Ki = 1848.0 nM 5.73
CHEMBL4112007 Ki = 2298.0 nM 5.64
CHEMBL4108986 Ki = 2883.0 nM 5.54
CHEMBL4112610 Ki = 5024.0 nM 5.30
CHEMBL4112412 Ki = 6374.0 nM 5.20
CHEMBL4115017 Ki = 6591.0 nM 5.18
CHEMBL4107302 Ki = 7324.0 nM 5.13
CHEMBL4109218 Ki = 7535.0 nM 5.12
CHEMBL3936595 Ki = 10000.0 nM 5.00
CHEMBL4114519 Ki > 10000.0 nM -
CHEMBL4112009 Ki > 10000.0 nM -
CHEMBL4110219 Ki > 10000.0 nM -
CHEMBL4115505 Ki > 10000.0 nM -