Assay Detail
Binding
CHEMBL2444624
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Inhibition of PHD2 (unknown origin) by HTRF assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel complex crystal structure of prolyl hydroxylase domain-containing protein 2 (PHD2): 2,8-Diazaspiro[4.5]decan-1-ones as potent, orally bioavailable PHD2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.90 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2042853 | — | — | 1 | 9.30 |
| CHEMBL2443222 | — | — | 1 | 9.00 |
| CHEMBL2443221 | — | — | 1 | 8.60 |
| CHEMBL2443211 | — | — | 1 | 8.40 |
| CHEMBL2443114 | — | — | 1 | 8.30 |
| CHEMBL2443129 | — | — | 1 | 8.10 |
| CHEMBL2443115 | — | — | 1 | 7.80 |
| CHEMBL2443213 | — | — | 1 | 7.80 |
| CHEMBL2443112 | — | — | 1 | 7.60 |
| CHEMBL2042997 | — | — | 1 | 7.60 |
| CHEMBL2443130 | — | — | 1 | 7.50 |
| CHEMBL2443113 | — | — | 1 | 7.40 |
| CHEMBL2443116 | — | — | 1 | 7.30 |
| CHEMBL2443118 | — | — | 1 | 7.10 |
| CHEMBL2443217 | — | — | 1 | 6.80 |
| CHEMBL2443218 | — | — | 1 | 6.70 |
| CHEMBL2443124 | — | — | 1 | 6.40 |
| CHEMBL2443126 | — | — | 1 | 6.30 |
| CHEMBL2443220 | — | — | 1 | 6.20 |
| CHEMBL2443128 | — | — | 1 | 6.20 |
| CHEMBL2443219 | — | — | 1 | 6.10 |
| CHEMBL2042128 | — | — | 1 | 6.00 |
| CHEMBL2443122 | — | — | 1 | 6.00 |
| CHEMBL2443120 | — | — | 1 | 5.90 |
| CHEMBL2443119 | — | — | 1 | 5.70 |
| CHEMBL2443127 | — | — | 1 | 5.70 |
| CHEMBL2443123 | — | — | 1 | 5.50 |
| CHEMBL2443125 | — | — | 1 | 5.50 |
| CHEMBL2443121 | — | — | 1 | 5.40 |
| CHEMBL2443212 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2042853 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL2443222 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2443221 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL2443211 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL2443114 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL2443129 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL2443115 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2443213 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2443112 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2042997 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2443130 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2443113 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL2443116 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL2443118 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL2443217 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL2443218 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL2443124 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL2443126 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2443220 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL2443128 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL2443219 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL2042128 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2443122 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2443120 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL2443119 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2443127 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2443123 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2443125 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2443121 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2443212 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL2443216 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2443215 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2443214 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2443117 | — | IC50 | > | 10000.0 | nM | - |