Assay Detail
Binding
CHEMBL5730231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Homogeneous Time Resolved Fluorescence Assay: The sGC cellular activator assay is performed in the presence and absence of 50% human serum (HS) using Chinese hamster ovary cells that have been stably transfected to express the human soluble guanylate cyclase alpha 1 and beta 1 subunits (sGC). Cells are preincubated with 40 microM 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), an sGC inhibitor, for one h in buffer containing 0.1% bovine serum albumin and 3-isobutyl-1-methylxanthine (IBMX). Concentration response curves are prepared for test compounds in DMSO. An intermediate dilution of the compounds is performed in either buffer containing IBMX or type AB HS containing IBMX. Diluted compounds are added to cells and they are incubated at room temperature for thirty min. cGMP is measured using a CisBio homogeneous time resolved fluorescence kit and the EC50 is calculated for each compound.
993
Total Activities
318
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Heterocyclic carboxylic acids as activators of soluble guanylate cyclase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 331 | 7.79 | 9.00 |
| kon | 331 | - | - |
| k_off | 331 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3925984 | — | — | 3 | 9.00 |
| CHEMBL3895428 | — | — | 3 | 9.00 |
| CHEMBL3904056 | — | — | 3 | 9.00 |
| CHEMBL3914172 | — | — | 3 | 9.00 |
| CHEMBL3940979 | — | — | 3 | 9.00 |
| CHEMBL3892047 | — | — | 3 | 9.00 |
| CHEMBL3931614 | — | — | 3 | 8.70 |
| CHEMBL3973541 | — | — | 3 | 8.70 |
| CHEMBL3932128 | — | — | 3 | 8.70 |
| CHEMBL4112354 | — | — | 3 | 8.70 |
| CHEMBL3927881 | — | — | 3 | 8.70 |
| CHEMBL3905803 | — | — | 3 | 8.70 |
| CHEMBL3896300 | — | — | 3 | 8.70 |
| CHEMBL3965913 | — | — | 3 | 8.70 |
| CHEMBL4109762 | — | — | 3 | 8.70 |
| CHEMBL3986854 | — | — | 3 | 8.70 |
| CHEMBL3952024 | — | — | 6 | 8.70 |
| CHEMBL3979282 | — | — | 3 | 8.70 |
| CHEMBL3906766 | — | — | 3 | 8.70 |
| CHEMBL3977406 | — | — | 3 | 8.70 |
| CHEMBL3894281 | — | — | 3 | 8.70 |
| CHEMBL3911781 | — | — | 9 | 8.70 |
| CHEMBL3930782 | — | — | 3 | 8.70 |
| CHEMBL3934762 | — | — | 3 | 8.70 |
| CHEMBL3939276 | — | — | 3 | 8.70 |
| CHEMBL3986578 | — | — | 3 | 8.70 |
| CHEMBL3901016 | — | — | 3 | 8.70 |
| CHEMBL3891521 | — | — | 6 | 8.52 |
| CHEMBL3976666 | — | — | 3 | 8.52 |
| CHEMBL3928977 | — | — | 3 | 8.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3895428 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3904056 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3925984 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3892047 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3940979 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3914172 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3901016 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3973541 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3952024 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3979282 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3986578 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3931614 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3965913 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3927881 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3896300 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3932128 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3986854 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3911781 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3930782 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3894281 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4112354 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3905803 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3977406 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4109762 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3934762 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3939276 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3906766 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3891521 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3911555 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3976666 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3891521 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3986811 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3986729 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3916990 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3906941 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4110239 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3901449 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3931703 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3928977 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3973307 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3905728 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3960701 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4111581 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4112328 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4111636 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3915441 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3961661 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3957197 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3901703 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3968935 | — | EC50 | = | 3.0 | nM | 8.52 |