| Unchecked |
K'a |
= |
1.0 |
|
Activation of cAMP-dependent protein kinase type I |
CHEMBL1126248 |
| cAMP-dependent protein kinase A |
K'a |
= |
1.0 |
|
Activation of cAMP-dependent protein kinase type II |
CHEMBL1126248 |
| Unchecked |
Specificity |
= |
1.0 |
|
Specificity for protein kinase-I and protein kinase-II |
CHEMBL1126248 |
| Unchecked |
Ka |
= |
8.0 |
M |
Compound was evaluated for activation of bovine heart protein kinase. |
CHEMBL1123904 |
| Phosphodiesterase 3B |
Km |
= |
530.0 |
nM |
Affinity for bovine heart phosphodiesterase |
CHEMBL1122040 |
| Unchecked |
Km |
= |
560.0 |
nM |
Affinity for rabbit lung phosphodiesterase |
CHEMBL1122040 |
| Unchecked |
Km |
= |
790.0 |
nM |
Affinity for rabbit kidney phosphodiesterase |
CHEMBL1122040 |
| Unchecked |
Ka' |
= |
1.0 |
|
Activate a partially purified type II cAMP-dependent protein kinase from bovine brain |
CHEMBL1121590 |
| Phosphodiesterase 4 |
Hydrolysis |
= |
1.0 |
|
Susceptibility to be hydrolysed by a partially purified cAMP phosphodiesterase from rabbit kidney |
CHEMBL1121590 |
| L1210 |
Inhibition |
= |
26.0 |
% |
Percent inhibition against L1210 cell line in mice. |
CHEMBL1122970 |
| P388 |
Inhibition |
= |
34.0 |
% |
Percent inhibition against P388 cell line in mice. |
CHEMBL1122970 |
| Vero |
Cytotoxicity |
|
|
|
In vitro cytotoxicity against Vero cells. |
CHEMBL1122970 |
| Vaccinia virus |
Virus rating |
= |
0.0 |
|
In vitro antiviral activity against Vaccinia virus strain Elstree was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Human herpesvirus 1 |
Virus rating |
= |
0.0 |
|
In vitro antiviral activity against Herpes simplex virus -1 strain KOS was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Human herpesvirus 2 |
Virus rating |
= |
0.2 |
|
In vitro antiviral activity against Herpes simplex virus -2 strain MS was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Human parainfluenza virus 3 |
Virus rating |
= |
0.0 |
|
In vitro antiviral activity against Para influenza virus type 3 strain C243 was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Vaccinia virus |
ED50 |
> |
5.0 |
mM l-1 |
Antiviral activity against Vaccinia virus strain Elstree was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Human herpesvirus 1 |
ED50 |
> |
5.0 |
mM l-1 |
Antiviral activity against Herpes simplex virus -1 strain KOS was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Human herpesvirus 2 |
ED50 |
> |
5.0 |
mM l-1 |
Antiviral activity against Herpes simplex virus -2 strain MS was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Human parainfluenza virus 3 |
ED50 |
> |
5.0 |
mM l-1 |
Antiviral activity against Para influenza virus type 3 strain C243 was evaluated in african green monkey kidney |
CHEMBL1122970 |
| Unchecked |
Km |
= |
200.0 |
nM |
Inhibition of Phosphodiesterase 7 |
CHEMBL1146771 |
| Phosphodiesterase 8A |
Km |
= |
50.0 |
nM |
Inhibition of Phosphodiesterase 8 |
CHEMBL1146771 |
| Phosphodiesterase 5A |
Km |
= |
150000.0 |
nM |
Inhibition of Phosphodiesterase 5 |
CHEMBL1146771 |
| Unchecked |
Km |
= |
0.63 |
|
Inhibition of bovine heart cAMP Phosphodiesterase |
CHEMBL1122020 |
| Unchecked |
Km |
= |
560.0 |
nM |
Inhibition of rabbit lung cAMP Phosphodiesterase |
CHEMBL1122020 |
| Unchecked |
Km |
= |
1300.0 |
nM |
Inhibition of bovine brain cAMP Phosphodiesterase |
CHEMBL1122020 |
| Alcohol dehydrogenase |
Ki |
= |
780000.0 |
nM |
Inhibition constant was evaluated against horse liver alcohol dehydrogenase |
CHEMBL1121822 |
| Unchecked |
K1/2 |
= |
3.8 |
uM |
Activation of olfactory CNG A2A41b channel expressed in HEK293 cells assessed as effect on half maximal current |
CHEMBL1148733 |
| Prelamin-A/C |
Potency |
= |
5.0 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of Lamin A Splicing. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase MLL |
Potency |
= |
125.9 |
nM |
PUBCHEM_BIOASSAY: qHTS Fluorescence Polarization Assay for Inhibitors of MLL CXXC domain - DNA interaction. (Class of assay: confirmatory) [Related pubchem assays: 2698 (Summary assay.)] |
CHEMBL1201862 |
| Unchecked |
Potency |
= |
31.6 |
nM |
PUBCHEM_BIOASSAY: Validation screen for inhibitors of Lassa infection. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Thyroid hormone receptor beta-1 |
Potency |
= |
0.6 |
nM |
PUBCHEM_BIOASSAY: Total Fluorescence Counterscreen for Inhibitors of the Interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Bloom syndrome protein |
Potency |
= |
3.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay for Inhibitors of Bloom's syndrome helicase (BLM). (Class of assay: confirmatory) [Related pubchem assays: 593 (Fluorescein region spectral profiling screen), 594 (Rhodamine region spectral profiling screen)] |
CHEMBL1201862 |
| Bloom syndrome protein |
Potency |
= |
3.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Bloom's syndrome helicase (BLM). (Class of assay: confirmatory) [Related pubchem assays: 593 (Fluorescein region spectral profiling screen), 2386 (Probe Development Summary for Inhibitors of Bloom's syndrome helicase (BLM)), 594 (Rhodamine region spectral profiling screen), 2364 (qHTS Validation Assay for Inhibitors of Bloom's syndrome helicase (BLM))] |
CHEMBL1201862 |
| Neuropeptide S receptor |
Potency |
= |
1584.9 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Antagonists of the Neuropeptide S Receptor: cAMP Signal Transduction. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
= |
141.3 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Lipid Storage Modulators. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Geminin |
Potency |
= |
22387.2 |
nM |
PUBCHEM_BIOASSAY: Validation screen for small molecules that induce DNA re-replication in MCF 10A normal breast cells. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Dopamine D1 receptor |
Potency |
|
19952.6 |
nM |
PUBCHEM_BIOASSAY: HTS Assay for Allosteric Agonists of the Human D1 Dopamine Receptor: Primary Screen for Antagonists. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488989, AID488993, AID488995] |
CHEMBL1201862 |
| Histone acetyltransferase GCN5 |
Potency |
|
39810.7 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of GCN5L2. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504398] |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Potency |
|
2818.4 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504404] |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Potency |
|
2377.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504404] |
CHEMBL1201862 |
| Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 |
Potency |
|
952.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay to Find Inhibitors of Pin1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504591] |
CHEMBL1201862 |
| Multidrug resistance-associated protein 4 |
Activity |
|
|
|
Substrates of transporters of clinical importance in the absorption and disposition of drugs, MRP4 |
CHEMBL1743141 |
| Regulator of G-protein signaling 4 |
Potency |
|
842.9 |
nM |
PUBCHEM_BIOASSAY: Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504856] |
CHEMBL1201862 |
| DNA polymerase eta |
Potency |
|
281.8 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of Polymerase Eta. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588636] |
CHEMBL1201862 |
| HEK293 |
Potency |
|
1635.3 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of binding or entry into cells for Lassa Virus. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463114, AID540249] |
CHEMBL1201862 |
| HEK293 |
Potency |
|
31.6 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of binding or entry into cells for Lassa Virus. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463114, AID540249] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
231.0 |
nM |
PUBCHEM_BIOASSAY: qHTS for inhibitors of binding or entry into cells for Marburg Virus. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463114, AID540249, AID540278] |
CHEMBL1201862 |
| Unchecked |
Km |
= |
710.0 |
nM |
Activity of bovine aortic PDE4 |
CHEMBL1914375 |
| Rap guanine nucleotide exchange factor 4 |
IC50 |
= |
48000.0 |
nM |
Competitive inhibition of Epac2 using fluorescent nucleotide analog 8-NBD-cAMP by fluorescence analysis |
CHEMBL2029310 |
| Rap guanine nucleotide exchange factor 4 |
Ratio IC50 |
= |
1.0 |
|
Competitive inhibition of Epac2 using fluorescent nucleotide analog 8-NBD-cAMP by fluorescence analysis relative to cAMP |
CHEMBL2029310 |
| Solute carrier family 22 member 6 |
Activity |
|
|
|
TP_TRANSPORTER: uptake in Xenopus laevis oocytes |
CHEMBL2074345 |
| Solute carrier family 22 member 8 |
Activity |
|
|
|
TP_TRANSPORTER: uptake in Xenopus laevis oocytes |
CHEMBL2074134 |
| Multidrug resistance-associated protein 4 |
Activity |
|
|
|
TP_TRANSPORTER: efflux in MRP4-expressing HepG2 cells |
CHEMBL2073783 |
| Solute carrier family 22 member 7 |
Activity |
|
|
|
TP_TRANSPORTER: uptake in OAT2-expressing EcR293 cells |
CHEMBL2073787 |
| ATP-binding cassette sub-family C member 11 |
Activity |
|
|
|
TP_TRANSPORTER: efflux in MRP8-1-expressing LLC-PK1 cells |
CHEMBL2073741 |
| Multidrug resistance-associated protein 5 |
Activity |
= |
35.5 |
% |
TP_TRANSPORTER: inhibition of cGMP uptake (cGMP: 5 uM, cAMP: 500 uM) in membrane vesicles from MRP5-expressing V79 cells |
CHEMBL2074325 |
| Multidrug resistance-associated protein 4 |
Activity |
= |
36.0 |
% |
TP_TRANSPORTER: inhibition of cGMP uptake (cGAMP: 1 uM, cAMP: 250 uM) in membrane vesicles from MRP4-expressing Sf9 cells |
CHEMBL2074199 |
| Multidrug resistance-associated protein 4 |
Activity |
= |
39.6 |
% |
TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 1 uM, cAMP: 300 uM) in membrane vesicles from MRP4-expressing Sf9 cells |
CHEMBL2074175 |
| Multidrug resistance-associated protein 4 |
Activity |
= |
48.5 |
% |
TP_TRANSPORTER: inhibition of MTX uptake (MTX: 20 uM, cAMP: 300 uM) in membrane vesicles from MRP4-expressing Sf9 cells |
CHEMBL2074469 |
| ATP-binding cassette sub-family C member 11 |
Activity |
= |
74.0 |
% |
TP_TRANSPORTER: ATP-dependent uptake of cAMP at a concentration of 10 uM in membrane vesicle from MRP8-expressing LLC-PK1 cells |
CHEMBL2074545 |
| Multidrug resistance-associated protein 5 |
Km |
= |
379000.0 |
nM |
TP_TRANSPORTER: uptake in membrane vesicles from MRP5-expressing V79 cells |
CHEMBL2074325 |
| Multidrug resistance-associated protein 4 |
Km |
= |
44500.0 |
nM |
TP_TRANSPORTER: uptake in membrane vesicles from MRP4-expressing Sf9 cells |
CHEMBL2074175 |
| Dopamine D1 receptor |
Potency |
|
366.3 |
nM |
PubChem BioAssay. HTS Assay for Allosteric Antagonists of the Human D2 Dopamine Receptor: Hit Validation in HTRF. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Streptavidin |
Activity |
|
|
|
Binding affinity to Streptomyces avidinii streptavidin at 4 mM using dye labeled Streptavidin binding aptamer by fluorescence spectral analysis method |
CHEMBL2202973 |
| Rap guanine nucleotide exchange factor 4 |
IC50 |
= |
40000.0 |
nM |
Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay |
CHEMBL2311500 |
| Rap guanine nucleotide exchange factor 4 |
IC50 |
= |
40000.0 |
nM |
Inhibition of EPAC2 (unknown origin) |
CHEMBL3259785 |
| C6 |
Activity |
= |
0.0 |
% |
Drug uptake in rat C6 cells assessed as morphologically differentiation at 10'-3 M after 20 mins by microscopy |
CHEMBL3272058 |
| C6 |
Activity |
= |
0.0 |
% |
Drug uptake in rat C6 cells assessed as morphologically differentiation at 10'-3 M after 50 mins by microscopy |
CHEMBL3272058 |
| C6 |
Activity |
= |
0.0 |
% |
Drug uptake in rat C6 cells assessed as morphologically differentiation at 10'-3 M after 90 mins by microscopy |
CHEMBL3272058 |
| C6 |
Activity |
= |
0.0 |
pmol/min |
Drug uptake in rat C6 cells assessed as cAMP level per of protein at 10'-3 M after 90 mins |
CHEMBL3272058 |
| NON-PROTEIN TARGET |
Activity |
|
|
|
Binding affinity to Triton-X 100 at 150 uM by 1H-NMR spectra analysis |
CHEMBL4396878 |
| Replicase polyprotein 1ab |
Inhibition |
= |
4.96 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
0.27 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| Rap guanine nucleotide exchange factor 3 |
Kd |
= |
4500.0 |
nM |
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by 8-NBD-cAMP based competitive fluorescence assay |
CHEMBL4602718 |
| SARS-CoV-2 |
Inhibition |
= |
0.27 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
