Assay Detail
Binding
CHEMBL3241464
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.84 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3236556 | — | — | 1 | 9.04 |
| CHEMBL3236554 | — | — | 1 | 8.96 |
| CHEMBL3236553 | — | — | 1 | 8.92 |
| CHEMBL3236552 | — | — | 1 | 8.85 |
| CHEMBL3236571 | — | — | 1 | 8.82 |
| CHEMBL3236579 | — | — | 1 | 8.77 |
| CHEMBL3236560 | — | — | 1 | 8.74 |
| CHEMBL3236576 | — | — | 1 | 8.64 |
| CHEMBL3236575 | — | — | 1 | 8.62 |
| CHEMBL3236561 | — | — | 1 | 8.54 |
| CHEMBL1093180 | — | — | 1 | 8.30 |
| CHEMBL3236548 | — | — | 1 | 8.30 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.30 |
| CHEMBL3236558 | — | — | 1 | 8.26 |
| CHEMBL3236577 | — | — | 1 | 8.10 |
| CHEMBL1915048 | — | — | 1 | 8.05 |
| CHEMBL3236578 | — | — | 1 | 8.03 |
| CHEMBL3236564 | — | — | 1 | 7.95 |
| CHEMBL3236570 | — | — | 1 | 7.92 |
| CHEMBL3236549 | JNJ-39758979 | 2.0 | 1 | 7.90 |
| CHEMBL185951 | — | — | 1 | 7.70 |
| CHEMBL3236550 | — | — | 1 | 7.70 |
| CHEMBL3236569 | — | — | 1 | 7.68 |
| CHEMBL3236568 | — | — | 1 | 7.68 |
| CHEMBL3236562 | — | — | 1 | 7.60 |
| CHEMBL3236555 | — | — | 1 | 7.60 |
| CHEMBL3236574 | — | — | 1 | 7.55 |
| CHEMBL3236565 | — | — | 1 | 7.52 |
| CHEMBL3236572 | — | — | 1 | 7.44 |
| CHEMBL3236557 | — | — | 1 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3236556 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL3236554 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3236553 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3236552 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3236571 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3236579 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3236560 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3236576 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3236575 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3236561 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL3236548 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1093180 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3236558 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3236577 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1915048 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3236578 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3236564 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL3236570 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3236549 | JNJ-39758979 | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL3236550 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL185951 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3236569 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3236568 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3236562 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3236555 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3236574 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3236565 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3236572 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3236557 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3236551 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3236582 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL3233048 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3236567 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL3236573 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3236581 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL3236559 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL3236563 | — | Ki | = | 328.0 | nM | 6.48 |
| CHEMBL3236580 | — | Ki | = | 357.0 | nM | 6.45 |
| CHEMBL3236566 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL3236584 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3236583 | — | Ki | > | 10000.0 | nM | - |