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Target
Potassium voltage-gated channel subfamily H member 1
Ligand
BDBM50012662
Substrate
n/a
Meas. Tech.
ChEMBL_1808111 (CHEMBL4307470)
IC50
490±n/a nM
Citation
 Oehlrich, D; Peschiulli, A; Tresadern, G; Van Gool, M; Vega, JA; De Lucas, AI; Alonso de Diego, SA; Prokopcova, H; Austin, N; Van Brandt, S; Surkyn, M; De Cleyn, M; Vos, A; Rombouts, FJR; Macdonald, G; Moechars, D; Gijsen, HJM; Trabanco, AA Evaluation of a Series of ?-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads. ACS Med Chem Lett 10:1159-1165 (2019) [PubMed]  Article 
Target
Name:
Potassium voltage-gated channel subfamily H member 1
Synonyms:
EAG | EAG channel 1 | EAG1 | Ether-a-go-go potassium channel 1 | KCNH1 | KCNH1_HUMAN | Potassium voltage-gated channel subfamily H member 1 | Synonyms=EAG | Voltage-gated potassium channel subunit Kv10.1 | h-eag | hEAG1
Type:
PROTEIN
Mol. Mass.:
111433.08
Organism:
Homo sapiens
Description:
ChEMBL_105708
Residue:
989
Sequence:
MTMAGGRRGLVAPQNTFLENIVRRSNDTNFVLGNAQIVDWPIVYSNDGFCKLSGYHRAEVMQKSSTCSFMYGELTDKDTIEKVRQTFENYEMNSFEILMYKKNRTPVWFFVKIAPIRNEQDKVVLFLCTFSDITAFKQPIEDDSCKGWGKFARLTRALTSSRGVLQQLAPSVQKGENVHKHSRLAEVLQLGSDILPQYKQEAPKTPPHIILHYCVFKTTWDWIILILTFYTAILVPYNVSFKTRQNNVAWLVVDSIVDVIFLVDIVLNFHTTFVGPAGEVISDPKLIRMNYLKTWFVIDLLSCLPYDVINAFENVDEVSAFMGDPGKIGFADQIPPPLEGRESQGISSLFSSLKVVRLLRLGRVARKLDHYIEYGAAVLVLLVCVFGLAAHWMACIWYSIGDYEIFDEDTKTIRNNSWLYQLAMDIGTPYQFNGSGSGKWEGGPSKNSVYISSLYFTMTSLTSVGFGNIAPSTDIEKIFAVAIMMIGSLLYATIFGNVTTIFQQMYANTNRYHEMLNSVRDFLKLYQVPKGLSERVMDYIVSTWSMSRGIDTEKVLQICPKDMRADICVHLNRKVFKEHPAFRLASDGCLRALAMEFQTVHCAPGDLIYHAGESVDSLCFVVSGSLEVIQDDEVVAILGKGDVFGDVFWKEATLAQSCANVRALTYCDLHVIKRDALQKVLEFYTAFSHSFSRNLILTYNLRKRIVFRKISDVKREEEERMKRKNEAPLILPPDHPVRRLFQRFRQQKEARLAAERGGRDLDDLDVEKGNVLTEHASANHSLVKASVVTVRESPATPVSFQAASTSGVPDHAKLQAPGSECLGPKGGGGDCAKRKSWARFKDACGKSEDWNKVSKAESMETLPERTKASGEATLKKTDSCDSGITKSDLRLDNVGEARSPQDRSPILAEVKHSFYPIPEQTLQATVLEVRHELKEDIKALNAKMTNIEKQLSEILRILTSRRSSQSPQELFEISRPQSPESERDIFGAS
  
Inhibitor
Name:
BDBM50012662
Synonyms:
CHEMBL3261075
Type:
Small organic molecule
Emp. Form.:
C21H17FN6O
Mol. Mass.:
388.3977
SMILES:
C[C@]1(Cn2cccc2C(N)=N1)c1cc(NC(=O)c2ccc(cn2)C#N)ccc1F |r,c:10|
Structure:
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